Pyrazole derivatives

ABSTRACT

Pyrazole compounds of formula  1! and their tautomers and salts: ##STR1## (wherein R 1  is an alkyl group, etc.; R 2  is a carboxyl group, etc.; R 3  is a halogen atom, an alkyl group, a phenyl group, etc.; R 4 , R 5  and R 6  each are a hydrogen atom, a halogen atom, etc.; R 7  is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). 
     The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

This is a Division of application Ser. No. 08/525,555 filed Sep. 29,1995 now U.S. Pat. No. 5,721,264 (U.S. National Stage of PCT/JP94/00587filed Apr. 7, 1994). The entire disclosure of the prior application(s)is hereby incorporated by reference herein in its entirety.

TECHNICAL FIELD

The present invention relates to novel pyrazole compounds and theirtautomers and salts, which are useful as antagonists against angiotensinII in remedy for various cardiovascular disorders, especially in remedyfor hypertension, cardiac insufficiency and venous insufficiency, aswell as in remedy for glaucoma, diabetic retinopathy and various centralnervous system disorders, such as anxiety neurosis, melancholia,hypomnesia, Alzheimer's disease or chronic renal insufficiency.

BACKGROUND ART

Renin-angiotensin system plays an important part in general bloodpressure regulation, and it substantially participates in themanifestation of hypertension and congestive cardiac insufficiency.Angiotensin II is an octapeptide hormone and is essentially formed inblood when angiotensin I which is a decapeptide hormone is cut byangiotensinase (angiotensin-converting enzyme; ACE). The ACE existslocally in the vascular endothelia of lung, kidney and other variousorgans. Angiotensin II which is a strong arterial angiotonic agent inrenin-angiotensin system acts on a specific receptor in the surfaces ofcell membranes. Therefore, one method for controlling renin-angiotensinsystem is to utilize the antagonistic effect against the angiotensin IIreceptor. It is known that some peptide analogues of angiotensin IIantagonistically block the receptor to thereby retard the effect of thehormone. However, since these peptide analogues have a partial agonisticactivity and are poorly absorbed by peroral administration, their use inexperimental and clinical purposes has heretofore been limited see M.Antonaccio, Clin. Exp. Hypertens., A4, 27-46 (1982)!.

Recently, some non-peptide compounds have been reported as antagonistsagainst angiotensin II see U.S. Pat. No. 4,207,324, No. 4,340,598, No.4,576,958, No. 4,582,847 and No. 4,880,804; European Patent ApplicationLaid-Opens No. 028,834, No. 245,637, No. 253,310, No. 291,969 and No.475,206; WO 93/17681 and WO 93/17682, etc.; A. T. Chiu, et al., Eur. J.Pharm. Exp. Therap., 157, 13-21 (1988); P. C. Wong, et al., J. Pharm.Exp. Therap., 247, 1-7 (1988); S. E. Laszlo, et al., J. Med. Chem.,1993, 36, 3207-3210, etc.!.

However, none of the above-mentioned U.S. patent specification, EuropeanPatent Application Laid-Open publications, PCT International Laid-OpenPatent Applications and the reports has disclosed the pyrazole compoundsand their tautomers and salts of the present invention.

The present invention relates to novel pyrazole compounds and theirtautomers and salts which are useful as antagonists against angiotensinII in remedy for various disorders such as hypertension, congestivecardiac insufficiency, chronic renal insufficiency, aldosteronism,hyper-intraocular pressure, etc.

DISCLOSURE OF INVENTION

The present inventors intensively investigated and researched and, as aresult, have unexpectedly found that the pyrazole compounds and theirtautomers and salts of the present invention, which are different fromall the compounds disclosed in the above-defined publications andliteratures, are useful as antagonists against angiotensin II capable ofbinding to not only AT₁ receptors but also AT₂ receptors, that they areextremely useful as antihypertensives and that they may be activeingredients in medicines for preventing and treating the above-mentioneddisorders such as congestive cardiac insufficiency, chronic renalinsufficiency, aldosteronism, hyper-intraocular pressure, etc. On thebasis of these findings, the present inventors have completed thepresent invention.

Specifically, the present invention relates to pyrazole compounds of thefollowing general formula 1! and their tautomers and salts: ##STR2##wherein R¹ represents a hydrogen atom, a C₁ -C₁₀ alkyl group {said alkylgroup is unsubstituted or substituted by one or more substituentsselected from a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group,NR⁸ R⁸ ' (in which R⁸ and R⁸ ' each independently represent a hydrogenatom, a C₁ -C₁₀ alkyl group or a C₆ -C₁₀ aromatic group), SR⁹ (in whichR⁹ has the same meaning as R⁸), a C₆ -C₁₀ aromatic group and aheterocyclic group}, a C₂ -C₁₀ alkenyl group {said alkenyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸ ' (inwhich R⁸ and R⁸ ' each independently have the same meanings as definedabove), SR⁹ (in which R⁹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}, a C₂ -C₁₀ alkynyl group{said alkynyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ ' each independently have thesame meanings as defined above), SR⁹ (in which R⁹ has the same meaningas defined above), a C₆ -C₁₀ aromatic group and a heterocyclic group}, aC₃ -C₁₀ cycloalkyl group {(said cycloalkyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ 'each independently have the same meanings as defined above), SR⁹ (inwhich R⁹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₃ -C₁₀ cycloalkenyl group {saidcycloalkenyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ ' each independently have thesame meanings as defined above), SR⁹ (in which R⁹ has the same meaningas defined above), a C₆ -C₁₀ aromatic group and a heterocyclic group}, aC₆ -C₁₀ aromatic group {said aromatic group is unsubstituted orsubstituted by one or more substituents selected from a C₁ -C₁₀ alkylgroup, a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸' (in which R⁸ and R⁸ ' each independently have the same meanings asdefined above), SR⁹ (in which R⁹ has the same meaning as defined above),a C₆ -C₁₀ aromatic group and a heterocyclic group}, a heterocyclic group{said heterocyclic group is unsubstituted or substituted by one or moresubstituents tuents selected from a C₁ -C₁₀ alkyl group, a halogen atom,a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ 'each independently have the same meanings as defined above), SR⁹ (inwhich R⁹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ acyl group {said acyl groupis unsubstituted or substituted by one or more substituents selectedfrom a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸ '(in which R⁸ and R⁸ ' each independently have the same meanings asdefined above), SR⁹ (in which R⁹ has the same meaning as defined above),a C₆ -C₁₀ aromatic group and a heterocyclic group}, a C₁ -C₁₀alkylcarbamoyl group {said alkylcarbamoyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ 'each independently have the same meanings as defined above), SR⁹ (inwhich R⁹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ alkoxycarbonyl group {saidalkoxycarbonyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR⁸ R⁸ ' (in which R⁸ and R⁸ ' each independently have thesame meanings as defined above), SR⁹ (in which R⁹ has the same meaningas defined above), a C₆ -C₁₀ aromatic group and a heterocyclic group},or a C₆ -C₁₀ aryloxycarbonyl group {said aryloxycarbonyl group isunsubstituted or substituted by one or more substituents selected from aC₁ -C₁₀ alkyl group, a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxygroup, NR⁸ R⁸ ' (in which R⁸ and R⁸ each independently have the samemeanings as defined above), SR⁹ (in which R⁹ has the same meaning asdefined above), a C₆ -C₁₀ aromatic group and a heterocyclic group};

R² represents a halogen atom, a nitro group, a cyano group, a formylgroup, a sulfonic acid group, a sulfonamide group, PO₂ H₂, PO₃ H₂, a5-tetrazolyl group, a 5-tetrazolylmethyl group, a 5-tetrazolylethylgroup, a C₁ -C₁₀ alkyl group {said alkyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰' each independently represent a hydrogen atom, a C₁ -C₁₀ alkyl group ora C₆ -C₁₀ aromatic group), SR¹¹ (in which R¹¹ has the same meaning asR¹⁰), a C₆ -C₁₀ aromatic group and a heterocyclic group)}, a C₂ -C₁₀alkenyl group {said alkenyl group is unsubstituted or substituted by oneor more substituents selected from a halogen atom, a hydroxyl group, aC₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' eachindependently have the same meanings as defined above), SR¹¹ (in whichR¹¹ has the same meaning as defined above), a C₆ -C₁₀ aromatic group anda heterocyclic group}, a C₂ -C₁₀ alkynyl group {said alkynyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (inwhich R¹⁰ and R¹⁰ ' each independently have the same meanings as definedabove), SR¹¹ (in which R¹¹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}, a C₃ -C₁₀ cycloalkylgroup {said cycloalkyl group is unsubstituted or substituted by one ormore substituents selected from a halogen atom, a hydroxyl group, a C₁-C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' each independentlyhave the same meanings as defined above), SR¹¹ (in which R¹¹ has thesame meaning as defined above), a C₆ -C₁₀ aromatic group and aheterocyclic group}, a C₃ -C₁₀ cycloalkenyl group {said cycloalkenylgroup is unsubstituted or substituted by one or more substituentsselected from a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group,NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' each independently have the samemeanings as defined above), SR¹¹ (in which R¹¹ has the same meaning asdefined above), a C₆ -C₁₀ aromatic group and a heterocyclic group}, a C₆-C₁₀ aromatic group {said aromatic group is unsubstituted or substitutedby one or more substituents selected from a C₁ -C₁₀ alkyl group, ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (inwhich R¹⁰ and R¹⁰ ' each independently have the same meanings as definedabove), SR¹¹ (in which R¹¹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}, a heterocyclic group{said heterocyclic group is unsubstituted or substituted by one or moresubstituents selected from a C₁ -C₁₀ alkyl group, a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰' each independently have the same meanings as defined above), SR¹¹ (inwhich R¹¹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ acyl group {said acyl groupis unsubstituted or substituted by one or more substituents selectedfrom a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰' (in which R¹⁰ and R¹⁰ ' each independently have the same meanings asdefined above), SR¹¹ (in which R¹¹ has the same meaning as definedabove), a C₆ -C₁₀ aromatic group and a heterocyclic group}, a C₁ -C₁₀alkylcarbamoyl group {said alkylcarbamoyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰' each independently have the same meanings as defined above), SR¹¹ (inwhich R¹¹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ alkoxycarbonyl group {saidalkoxycarbonyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' each independently havethe same meanings as defined above), SR¹¹ (in which R¹¹ has the samemeaning as defined above), a C₆ -C₁₀ aromatic group and a heterocyclicgroup}, a C₆ -C₁₀ aryloxycarbonyl group {said aryloxycarbonyl group isunsubstituted or substituted by one or more substituents selected from aC₁ -C₁₀ alkyl group, a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxygroup, NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' each independently have thesame meanings as defined above), SR¹¹ (in which R¹¹ has the same meaningas defined above), a C₆ -C₁₀ aromatic group and a heterocyclic group},(CH₂)m¹ COX¹ R¹² in which m¹ represents 0, 1 or 2; R¹² represents ahydrogen atom or a C₁ -C₁₀ alkyl group {said alkyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (inwhich R¹⁰ and R¹⁰ ' each independently have the same meanings as definedabove), SR¹¹ (in which R¹¹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}; X¹ represents an oxygenatom, a sulfur atom or NR¹³ (in which R¹³ has the same meaning as R¹⁰)!,(CH₂)n¹ X² R¹⁴ in which n¹ represents 0, 1 or 2; R¹⁴ represents ahydrogen atom, a C₁ -C₁₀ alkyl group {said alkyl group is unsubstitutedor substituted by one or more substituents selected from a halogen atom,a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁰ R¹⁰ ' (in which R¹⁰ andR¹⁰ ' each independently have the same meanings as defined above), SR¹¹(in which R¹¹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, or a C₁ -C₁₀ acyl group {said acylgroup is unsubstituted or substituted by one or more substituentsselected from a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group,NR¹⁰ R¹⁰ ' (in which R¹⁰ and R¹⁰ ' each independently have the samemeanings as defined above), SR¹¹ (in which R¹¹ has the same meaning asdefined above), a C₆ -C₁₀ aromatic group and a heterocyclic group}; X²represents an oxygen atom, S(O)n² (in which n² represents 0, 1, 2 or 3),or NR¹⁶ {in which R¹⁵ has the same meaning as R¹² or represents SO₂ R¹⁶(in which R¹⁶ represents a C₁ -C₁₀ alkyl group which is unsubstituted orsubstituted by halogen atom(s)}!, or an oxadiazole group of: ##STR3##(wherein R¹⁷, R¹⁷ ' and R¹⁷⁻ each have the same meanings as R¹⁰); R³represents a halogen atom, a hydroxyl group, a nitro group, a cyanogroup, a formyl group, a guanidino group, an amidino group, a sulfonicacid group, a sulfonamide group, PO₂ H₂, PO₃ H₂, a 5-tetrazolyl group, a5-tetrazolylmethyl group, a 5-tetrazolylethyl group, a C₁ -C₁₀ alkylgroup {said alkyl group is unsubstituted or substituted by one or moresubstituents ents selected from a halogen atom, a hydroxyl group, a C₁-C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independentlyrepresent a hydrogen atom, a C₁ -C₁₀ alkyl group or a C₆ -C₁₀ aromaticgroup), SR¹⁹ (in which R¹⁹ has the same meaning as R¹⁸), a C₆ -C₁₀aromatic group and a heterocyclic group}, a C₂ -C₁₀ alkenyl group {saidalkenyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independently havethe same meanings as defined above), SR¹⁹ (in which R¹⁹ has the samemeaning as defined above), a C₆ -C₁₀ aromatic group and a heterocyclicgroup}, a C₂ -C₁₀ alkynyl group {said alkynyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸' each independently have the same meanings as mentioned above), SR¹⁹(in which R¹⁹ has the same meaning as mentioned above), a C₆ -C₁₀aromatic group and a heterocyclic group}, a C₃ -C₁₀ cycloalkyl group{said cycloalkyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independently havethe same meanings as defined above), SR¹⁹ (in which R¹⁹ has the samemeaning as defined above), a C₆ -C₁₀ aromatic group and a heterocyclicgroup}, a C₃ -C₁₀ cycloalkenyl group {said cycloalkenyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (inwhich R¹⁸ and R¹⁸ ' each independently have the same meanings as definedabove), SR¹⁹ (in which R¹⁹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}, a C₆ -C₁₀ aromatic groupsaid aromatic group is unsubstituted or mono-substituted topenta-substituted by one or more substituents selected from a halogenatom, a hydroxyl group, a nitro group, a cyano group, a formyl group, aguanidino group, an amidino group, a sulfonic acid group, a sulfonamidegroup, PO₂ H₂, PO₃ H₂, a 5-tetrazolyl group, a C₁ -C₁₀ alkyl group {saidalkyl group is unsubstituted or substituted by one or more substituentsselected from a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group,NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independently have the samemeanings as defined above), SR¹⁹ (in which R¹⁹ has the same meaning asdefined above), a C₆ -C₁₀ aromatic group and a heterocyclic group}, a C₂-C₁₀ alkenyl group {said alkenyl group is unsubstituted or substitutedby one or more substituents selected from a halogen atom, a hydroxylgroup, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' eachindependently have the same meanings as defined above), SR¹⁹ (in whichR¹⁹ has the same meaning as defined above), a C₆ -C₁₀ aromatic group anda heterocyclic group}, a C₃ -C₁₀ cycloalkyl group {said cycloalkyl groupis unsubstituted or substituted by one or more substituents selectedfrom a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸' (in which R¹⁸ and R¹⁸ ' each independently have the same meanings asdefined above), SR¹⁹ (in which R¹⁹ has the same meaning as definedabove), a C₆ -C₁₀ aromatic group and a heterocyclic group}, (CH₂)m² COX³R²⁰ in which m² represents 0, 1 or 2; R²⁰ represents a hydrogen atom ora C₁ -C₁₀ alkyl group {said alkyl group is unsubstituted or substitutedby one or more substituents selected from a halogen atom, a hydroxylgroup, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' eachindependently have the same meanings as defined above), SR¹⁹ (in whichR¹⁹ has the same meaning as defined above), a C₆ -C₁₀ aromatic group anda heterocyclic group}; X³ represents an oxygen atom, a sulfur atom orNR²¹ (in which R²¹ has the same meaning as R¹⁸)!, (CH₂)n³ X⁴ R²² inwhich n³ represents 0, 1 or 2; R²² represents a hydrogen atom, a C₁ -C₁₀alkyl group {said alkyl group is unsubstituted or substituted by one ormore substituents selected from a halogen atom, a hydroxyl group, a C₁-C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independentlyhave the same meanings as defined above), SR¹⁹ (in which R¹⁹ has thesame meaning as defined above), a C₆ -C₁₀ aromatic group and aheterocyclic group}, or a C₁ -C₁₀ acyl group {said acyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (inwhich R¹⁸ and R¹⁸ ' each independently have the same meanings as definedabove), SR¹⁹ (in which R¹⁹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}; X⁴ represents an oxygenatom, S(O)n⁴ (in which n⁴ represents 0, 1, 2 or 3), or NR²³ {in whichR²³ has the same meaning as R²⁰ or represents SO₂ R²⁴ (in which R²⁴represents a C₁ -C₁₀ alkyl group which is unsubstituted or substitutedby halogen atom(s))}!, a C₆ -C₁₀ aromatic group, a heterocyclic groupand an oxadiazole group represented by R² !, a heterocyclic group {saidheterocyclic group is unsubstituted or substituted by one or moresubstituents selected from a C₁ -C₁₀ alkyl group, a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸' each independently have the same meanings as defined above), SR¹⁹ (inwhich R¹⁹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ acyl group {said acyl groupis unsubstituted or substituted by one or more substituents selectedfrom a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸' (in which R¹⁸ and R¹⁸ ' each independently have the same meanings asdefined above), SR¹⁹ (in which R¹⁹ has the same meaning as definedabove), a C₆ -C₁₀ aromatic group and a heterocyclic group}, a C₁ -C₁₀alkylcarbamoyl group {said alkylcarbamoyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸' each independently have the same meanings as defined above), SR¹⁹ (inwhich R¹⁹ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ alkoxycarbonyl group {saidalkoxycarbonyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group, a C₁ -C₁₀alkoxy group, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independently havethe same meanings as defined above), SR¹⁹ (in which R¹⁹ has the samemeaning as defined above), a C₆ -C₁₀ aromatic group and a heterocyclicgroup}, a C₆ -C₁₀ aryloxycarbonyl group {said aryloxycarbonyl group isunsubstituted or substituted by one or more substituents selected from aC₁ -C₁₀ alkyl group, a halogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxygroup, NR¹⁸ R¹⁸ ' (in which R¹⁸ and R¹⁸ ' each independently have thesame meanings as defined above), SR¹⁹ (in which R¹⁹ has the same meaningas defined above), a C₆ -C₁₀ aromatic group and a heterocyclic group},(CH₂)m³ COX⁵ R²⁶ {in which m³ represents 0, 1 or 2; R²⁵ has the samemeaning as R¹ ; X⁵ represents a covalent bond, an oxygen atom, a sulfuratom or NR²⁶ (in which R²⁶ has the same meaning as R¹⁸)}, (CH₂)n⁵ X⁶ R²⁷in which n⁵ represents 0, 1 or 2; R²⁷ has the same meaning as R¹, or itrepresents a nitro group, a cyano group, a formyl group, a guanidinogroup, an amidino group, a sulfonic acid group, a sulfonamide group, PO₂H₂, PO₃ H₂, a 5-tetrazolyl group, or represents an oxadiazole grouprepresented by R² ; X⁶ represents a covalent bond, an oxygen atom,S(O)n⁶ (in which n⁶ represents 0, 1, 2 or 3), or NR²⁸ {in which R²⁸ hasthe same meaning as R²⁰ or represents SO₂ R²⁹ (in which R²⁹ represents aC₁ -C₁₀ alkyl group is unsubstituted or substituted by halogenatom(s))}!, or (CH₂)m⁴ X⁷ COR³⁰ in which m⁴ represent 0, 1 or 2; R³⁰represents a hydrogen atom, a C₁ -C₁₀ alkyl group {said alkyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR¹⁸ R¹⁸ ' (inwhich R¹⁸ and R¹⁸ ' each independently have the same meanings as definedabove), SR¹⁹ (in which R¹⁹ has the same meaning as defined above), a C₆-C₁₀ aromatic group and a heterocyclic group}, or NR³¹ R³¹ ' (in whichR³¹ and R³¹ ' each independently have the same meanings as R¹⁸); X⁷represents an oxygen atom, a sulfur atom or NR³² (in which R³² has thesame meaning as R¹⁸)!; R⁴, R⁵ and R⁶ each independently represent ahydrogen atom, a halogen atom, a hydroxyl group, a nitro group, a cyanogroup, a formyl group, a guanidino group, an amidino group, a carboxylgroup, a sulfonic acid group, a sulfonamide group, PO₂ H₂, PO₃ H₂, a5-tetrazolyl group, a C₁ -C₁₀ alkyl group {said alkyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group, a C₁ -C₁₀ alkoxy group, NR³³ R³³ ' (inwhich R³³ and R³³ ' each independently represent a hydrogen atom, a C₁-C₁₀ alkyl group or a C₆ -C₁₀ aromatic group), SR³⁴ (in which R³⁴ hasthe same meaning as R³³), a C₆ -C₁₀ aromatic group and a heterocyclicgroup}, a C₁ -C₁₀ acyl group {said acyl group is unsubstituted orsubstituted by one or more substituents selected from a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR³³ R³³ ' (in which R³³ and R³³' each independently have the same meanings as defined above), SR³⁴ (inwhich R³⁴ has the same meaning as defined above), a C₆ -C₁₀ aromaticgroup and a heterocyclic group}, a C₁ -C₁₀ alkoxy group, or NR³³ R³³ '(in which R³³ and R³³ ' each independently have the same meanings asdefined above);

R⁷ represents a carboxyl group (said carboxyl group may be protected bya methyl group, a t-butyl group or the like), a sulfonic acid group, asulfonamide group, PO₂ H₂, PO₃ H₂, a 5-tetrazolyl group (said tetrazolylgroup may be protected by a triphenylmethyl group, a methoxymethylgroup, a methoxyethoxymethyl group, a benzyl group or the like), anoxadiazole group represented by R², X⁸ R³⁵ {in which R³⁵ has the samemeaning as R¹² ; X⁸ represents an oxygen atom, a sulfur atom, NR³⁶ (inwhich R³⁶ has the same meaning as R³³), or SO₂ R³⁷ (in which R³⁷represents a C₁ -C₁₀ alkyl group (said alkyl group is unsubstituted orsubstituted by halogen atom(s))}, a heterocyclic group {saidheterocyclic group is unsubstituted or substituted by one or moresubstituents selected from a C₁ -C₁₀ alkyl group, a halogen atom, ahydroxyl group, a C₁ -C₁₀ alkoxy group, NR³⁸ R³⁸ ' (in which R³⁸ and R³⁸' each independently represent a hydrogen atom, a C₁ -C₁₀ alkyl group ora C₆ -C₁₀ aromatic group), SR³⁹ (in which R³⁹ has the same meaning asR³⁸), a C₆ -C₁₀ aromatic group and a heterocyclic group}, or asubstituent of: ##STR4## X represents a nitrogen atom or N→O; Y and Zeach independently represent a nitrogen atom or CR⁴⁰ (in which R⁴⁰ hasthe same meaning as R⁴);

A represents (CR⁴¹ R⁴¹ ')m⁷ -L--(CR⁴² R⁴² ')n⁷ {in which m⁷ and n⁷ eachindependently represent 0, 1, 2 or 3; R⁴¹, R⁴¹ ', R⁴² and R⁴² ' eachindependently have the same meanings as R⁴ ;

L represents a covalent bond, an oxygen atom, a carbonyl group, NR⁴³ (inwhich R⁴³ represents a hydrogen atom, a C₁ -C₁₀ alkyl group or a C₆ -C₁₀aromatic group), NR⁴⁴ --CO (in which R⁴⁴ has the same meaning as R⁴³),CO--NR⁴⁶ (in which R⁴⁵ has the same meaning as R⁴³), S(O)m⁶ (in which m⁶represents 0, 1 or 2), NR⁴⁶ --CO--NR⁴⁷ (in which R⁴⁶ and R⁴⁷ eachindependently have the same meanings as R⁴³), CR⁴⁸ ═CR⁴⁹ (in which R⁴⁸and R⁴⁹ each independently have the same meanings as R⁴³), C.tbd.C, orNR⁵⁰ --NR⁵¹ (in which R⁵⁰ and R⁵¹ each independently have the samemeanings as R⁴³)};

D represents a C₆ -C₁₀ aromatic group (said aromatic group isunsubstituted or mono-substituted to penta-substituted by one or moresubstituents represented by R³);

E represents (CR⁵² R⁵³)m⁶ X⁹ {in which m⁶ represents 0, 1 or 2; R⁵² andR⁵³ each independently have the same meanings as R⁴ ;

X⁹ represents a covalent bond, an oxygen atom, a sulfur atom or NR⁶⁴ (inwhich R⁵⁴ represents a hydrogen atom, a C₁ -C₁₀ alkyl group or a C₆ -C₁₀aromatic group)};

G represents a covalent bond, an oxygen atom, S(O)m⁸ (in which m⁸represents 0, 1 or 2), NR⁵⁵ (in which R⁵⁵ represents a hydrogen atom, aC₁ -C₁₀ alkyl group or a C₆ -C₁₀ aromatic group), a carbonyl group,(CR⁵⁵ R⁵⁶)n⁸ (in which n⁸ represents 0, 1 or 2; R⁵⁵ and R⁵⁶ eachindependently represent a hydrogen atom, a C₁ -C₁₀ alkyl group or a C₆-C₁₀ aromatic group), CO--NR⁵⁷ (in which R⁵⁷ represents a hydrogen atom,a C₁ -C₁₀ alkyl group or a C₆ -C₁₀ aromatic group), or NR⁵⁸ --CO (inwhich R⁵⁸ represents a hydrogen atom, a C₁ -C₁₀ alkyl group or a C₆ -C₁₀aromatic group)!.

Examples of the substituents in the compounds of the above-mentionedformula 1! are mentioned below.

C₁ -C₁₀ alkyl group includes, for example, a methyl group, an ethylgroup, an n-propyl group, an i-propyl group, an n-butyl group, asec-butyl group, a t-butyl group, an n-pentyl group, a neopentyl group,a hexyl group, etc.

C₂ -C₁₀ alkenyl group includes, for example, a vinyl group, an allylgroup, an i-propenyl group, a 1-butenyl group, a 2-butenyl group, a3-butenyl group, a 1,3-butadienyl group, a 1-pentenyl group, a2-pentenyl group, a 3-pentenyl group, a 4-pentenyl group, a 1-hexenylgroup, a 2-hexenyl group, a 3-hexenyl group, a 4-hexenyl group, a5-hexenyl group, etc.

C₂ -C₁₀ alkynyl group includes, for example, an ethynyl group, a1-propynyl group, a 2-propynyl group, a 1-butynyl group, a 2-butynylgroup, a 3-butynyl group, a 1-pentynyl group, a 2-pentynyl group, a3-pentynyl group, a 4-pentynyl group, a 1-hexynyl group, a 2-hexynylgroup, a 3-hexynyl group, a 4-hexynyl group, a 5-hexynyl group, etc.

C₃ -C₁₀ cycloalkyl group is meant to also include an alkylcycloalkylgroup and a cycloalkylalkyl group, for example, including a c-propylgroup, a c-butyl group, a c-pentyl group, a c-hexyl group, a4-methyl-c-hexyl group, a c-propylmethyl group, etc.

C₈ -C₁₀ cycloalkenyl group is meant to also include an alkylcycloalkenylgroup and a cycloalkenylalkyl group, for example, including a1-c-pentenyl group, a 2-c-pentenyl group, a 2,4-c-pentadienyl group, a1-c-hexenyl group, a 2-c-hexenyl group, a 3-c-hexenyl group, a4-methyl-1-c-hexenyl group, a 1-c-pentenylmethyl group, etc.

C₆ -C₁₀ aromatic group includes, for example, a phenyl group, a1-indenyl group, a 2-indenyl group, a 3-indenyl group, a 4-indenylgroup, a 5-indenyl group, a 6-indenyl group, a 7-indenyl group, a1-naphthyl group, a 2-naphthyl group, a 1-tetrahydronaphthyl group, a2-tetrahydronaphthyl group, a 5-tetrahydronaphthyl group, a6-tetrahydronaphthyl group, a 1-pentalenyl group, a 2-pentalenyl group,a 1-azulenyl group, a 2-azulenyl group, a 4-azulenyl group, a 5-azulenylgroup, a 6-azulenyl group, etc.

Heterocyclic group is meant to include an aromatic heterocyclic groupand a non-aromatic heterocyclic group.

As aromatic heterocyclic groups, mentioned are a 5-membered to7-membered mono-heterocyclic group and a condensed bi-heterocyclic grouphaving from 8 to 10 ring-constituting atoms, which contain from 1 to 5hetero-atoms chosen from among oxygen, nitrogen and/or sulfur atoms.

As non-aromatic heterocyclic groups, mentioned are a 3-membered to7-membered mono-heterocyclic group, a condensed bi-heterocyclic grouphaving from 6 to 10 ring-constituting atoms and a crosslinkedheterocyclic group having up to 10 ring-constituting atoms, whichcontain from 1 to 5 hetero-atoms chosen from among oxygen, nitrogenand/or sulfur atoms.

Aromatic heterocyclic group includes, for example, a 2-thienyl group, a3-thienyl group, a 2-furyl group, a 3-furyl group, a 2-pyranyl group, a3-pyranyl group, a 4-pyranyl group, a 2-benzofuranyl group, a3-benzofuranyl group, a 4-benzofuranyl group, a 5-benzofuranyl group, a6-benzofuranyl group, a 7-benzofuranyl group, a 1-isobenzofuranyl group,a 4-isobenzofuranyl group, a 5-isobenzofuranyl group, a 2-benzothienylgroup, a 3-benzothienyl group, a 4-benzothienyl group, a 5-benzothienylgroup, a 6-benzothienyl group, a 7-benzothienyl group, a1-isobenzothienyl group, a 4-isobenzothienyl group, a 5-isobenzothienylgroup, a 2-chromenyl group, a 3-chromenyl group, a 4-chromenyl group, a5-chromenyl group, a 6-chromenyl group, a 7-chromenyl group, an8-chromenyl group, a 1-pyrrolyl group, a 2-pyrrolyl group, a 3-pyrrolylgroup, a 1-imidazolyl group, a 2-inidazolyl group, a 4-imidazolyl group,a 1-pyrazolyl group, a 3-pyrazolyl group, a 4-pyrazolyl group, a2-thiazolyl group, a 4-thiazolyl group, a 5-thiazolyl group, a3-isothiazolyl group, a 4-isothiazolyl group, a 5-isothiazolyl group, a2-oxazolyl group, a 4-oxazolyl group a 5-oxazolyl group, a 3-isoxazolylgroup, a 4-isoxazolyl group, a 5-isoxazolyl group, a 2-pyridyl group, a3-pyridyl group, a 4-pyridyl group, a 2-pyrazinyl group, a 2-pyrimidinylgroup, a 4-pyrimidinyl group, a 5-pyrimidinyl group, a 3-pyridazinylgroup, a 4-pyridazinyl group, a 1-indolidinyl group, a 2-indolidinylgroup, a 3-indolidinyl group, a 5-indolidinyl group, a 6-indolidinylgroup, a 7-indolidinyl group, an 8-indolidinyl group, a 1-isoindolylgroup, a 4-isoindolyl group, a 5-isoindolyl group, a 1-indolyl group, a2-indolyl group, a 3-indolyl group, a 4-indolyl group, a 5-indolylgroup, a 6-indolyl group, a 7-indolyl group, a 1-indazolyl group, a2-indazolyl group, a 3-indazolyl group, a 4-indazolyl group, a5-indazolyl group, a 6-indazolyl group, a 7-indazolyl group, a 1-purinylgroup, a 2-purinyl group, a 3-purinyl group, a 6-purinyl group, a7-purinyl group, an 8-purinyl group, a 2-quinolyl group, a 3-quinolylgroup, a 4-quinolyl group, a 5-quinolyl group, a 6-quinolyl group, a7-quinolyl group, an 8-quinolyl group, a 1-isoquinolyl group, a3-isoquinolyl group, a 4-isoquinolyl group, a 5-isoquinolyl group, a6-isoquinolyl group, a 7-isoquinolyl group, an 8-isoquinolyl group, a1-phthalazinyl group, a 5-phthalazinyl group, a 6-phthalazinyl group, a2-naphthyridinyl group, a 3-naphthyridinyl group, a 4-naphthyridinylgroup, a 2-quinoxalinyl group, a 5-quinoxalinyl group, a 6-quinoxalinylgroup, a 2-quinazolinyl group, a 4-quinazolinyl group, a 5-quinazolinylgroup, a 6-quinazolinyl group, a 7-quinazolinyl group, an 8-quinazolinylgroup, a 3-cinnolinyl group, a 4-cinnolinyl group, a 5-cinnolinyl group,a 6-cinnolinyl group, a 7-cinnolinyl group, an 8-cinnolinyl group, a2-pteridinyl group, a 4-pteridinyl group, a 6-pteridinyl group, a7-pteridinyl group, a 3-furazanyl group, etc. These groups isunsubstituted or substituted by one or more substituents selected from ahydroxyl group, a halogen atom, an oxo group (═O), an amino group, analkyl group, etc.

Non-aromatic heterocyclic group includes, for example, a 2-chromanylgroup, a 3-chromanyl group, a 4-chromanyl group, a 5-chromanyl group, a6-chromanyl group, a 7-chromanyl group, an 8-chromanyl group, a1-isochromanyl group, a 3-isochromanyl group, a 4-isochromanyl group, a5-isochromanyl group, a 6-isochromanyl group, a 7-isochromanyl group, an8-isochromanyl group, a 1-pyrrolidinyl group, a 2-pyrrolidinyl group, a3-pyrrolidinyl group, a 1-pyrrolinyl group, a 2-pyrrolinyl group, a3-pyrrolinyl group, a 4-pyrrolinyl group, a 5-pyrrolinyl group, a1-imidazolidinyl group, a 2-imidazolidinyl group, a 4-imidazolidinylgroup, a 1-imidazolinyl group, a 2-imidazolinyl group, a 4-imidazolinylgroup, a 1-pyrazolidinyl group, a 3-pyrazolidinyl group, a4-pyrazolidinyl group, a 1-pyrazolinyl group, a 2-pyrazolinyl group, a3-pyrazolinyl group, a 4-pyrazolinyl group, a 5-pyrazolinyl group, a1-piperidyl group, a 2-piperidyl group, a 3-piperidyl group, a4-piperidyl group, a 1-piperazinyl group, a 2-piperazinyl group, a3-piperazinyl group, a 1-indolinyl group, a 2-indolinyl group, a3-indolinyl group, a 4-indolinyl group, a 5-indolinyl group, a6-indolinyl group, a 7-indolinyl group, a 1-isoindolinyl group, a2-isoindolinyl group, a 4-isoindolinyl group, a 5-isoindolinyl group, a2-quinuclidinyl group, a 3-quinuclidinyl group, a 4-quinuclidinyl group,a 2-morpholinyl group, a 3-morpholinyl group, a 4-morpholinyl group, a1-azetidinyl group, a 2-azetidinyl group, a 3-azetidinyl group, a1-azetidinonyl group, a 3-azetidinonyl group, a 4-azetidinonyl group,etc. These groups may optionally be substituted by one or moresubstituents selected from a hydroxyl group, a halogen atom, an oxogroup (═O), an amino group, an alkyl group, etc.

C₁ -C₁₀ acyl group includes, for example, a formyl group, an acetylgroup, a propionyl group, a butyryl group, an isobutyryl group, avaleryl group, an isovaleryl group, a pivaloyl group, an acryloyl group,a propioloyl group, a methacryloyl group, a crotonoyl group, a benzoylgroup, a 2-furoyl group, a 3-furoyl group, a 2-thenoyl group, a3-thenoyl group, a nicotinoyl group, a cyclopropylcarbonyl group, ahydroatropoyl group, a cinnamoyl group, etc.

C₁ -C₁₀ alkylcarbamoyl group includes, for example, an N-methylcarbamoylgroup, an N,N-dimethylcarbamoyl group, an N-ethylcarbamoyl group, anN-propylcarbamoyl group, an N-butyl-N-methylcarbamoyl group, anN-phenylcarbamoyl group, a succinamoyl group, etc.

C₁ -C₁₀ alkoxycarbonyl group includes, for example, a methoxycarbonylgroup, an ethoxycarbonyl group, an n-propoxycarbonyl group, ani-propoxycarbonyl group, an n-butoxycarbonyl group, a sec-butoxycarbonylgroup, a t-butoxycarbonyl group, a benzyloxycarbonyl group, etc.

C₆ -C₁₀ aryloxycarbonyl group includes, for example, a phenoxycarbonylgroup, a 1-naphthyloxycarbonyl group, a 2-naphthyloxycarbonyl group, an8-quinolinoxycarbonyl group, etc.

C₁ -C₁₀ alkoxy group includes, for example, a methoxy group, an ethoxygroup, an n-propoxy group, an i-propoxy group, an n-butoxy group, asec-butoxy group, a t-butoxy group, a benzyloxy group, a phenoxy group,a 1-naphthyloxy group, a 2-naphthyloxy group, an 8-quinolinoxy group,etc.

Halogen atom includes fluorine atom, chlorine atom, bromine atom andiodine atom.

Pyrazole compounds of formula 1! and their tautomers and salts of thepresent invention may be produced according to the methods mentionedbelow. ##STR5## (In these formulae, R², R³, R⁴, R⁵, R⁶, R⁷, A, D, E, G,X, Y and Z have the same meanings as defined above; V represents ahalogen atom such as chlorine atom, bromine atom, iodine atom, etc., ora leaving group such as a methanesulfonyloxy group, apara-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group,etc.)

According to the reaction scheme (1), a compound of the formula 2b! isreacted with a compound of formula 3a! to give a compound of the formula5! and, if necessary, the obtained compound is deprotected to produce acompound of the formula 1! wherein R¹ is a hydrogen atom.

Usually, the reaction may be effected in the presence of an inorganicbase such as potassium carbonate, sodium carbonate, lithium carbonate,potassium hydrogencarbonate, sodium hydrogencarbonate, lithiumhydroxide, etc. Apart from the above-mentioned inorganic bases, alsoemployable are metal hydrides such as sodium hydride, potassium hydride,n-butyl lithium, etc.; metal alkoxides such as sodium methoxide, sodiumethoxide, potassium t-butoxide, etc.; metal amides such as sodium amide,lithium di-isopropylamide, lithium hexamethyldisilazide, lithium2,2,6,6-tetramethylpiperidide, etc.; and organic bases such astrimethylamine, triethylamine, pyridine, diisopropylethylamine, etc.

Any reaction solvent that does not participate in the reaction may beemployable. Usually, used are hydrocarbon solvents such as benzene,toluene, hexane, etc.; ether solvents such as tetrahydrofuran, diethylether, 1,4-dioxane, etc.; amide solvents such as formamide,N,N-dimethylformamide, N,N-dimethylacetamide, N-methylpyrrolidone, etc.;alcohol solvents such as methanol, ethanol, propanol, etc.;halogen-containing solvents such as chloroform, methylene chloride,ethylene dichloride, etc.; other solvents such as acetonitrile,dimethylsulfoxide, etc.; water; and mixed solvents comprising two ormore of them.

The reaction temperature may be within the range of from -78° C. to theboiling point of the solvent used in the reaction.

The molar ratio of the starting compounds may be defined freely. Ingeneral, the compound of the formula 2b! may be reacted with thecompound of formula 3a! in an amount of from 0.8 to 1.5 times by mol thelatter.

The deprotection may be effected by known methods. For example, themethyl ester or ethyl ester residue in the protected intermediate may beremoved by reacting the intermediate with sodium hydroxide, potassiumhydroxide or the like in a water-alcohol solvent while cooling with iceor at room temperature or lower. The triphenylmethyl group in the samemay be removed by treating the intermediate with an aqueous acetic acidor hydrochloric acid-ethanol or with ethanol under reflux.

The benzyl group may be removed by hydrogenolysis of the protectedintermediate with hydrogen gas, using a Pd-carbon catalyst; and themethoxymethyl ether residue may be removed by treating the intermediatewith hydrochloric acid-ethanol. ##STR6## (In these formulae, R², R³, R⁴,R⁵, R⁶, R⁷, A, D, E, G, X, Y, Z and V have the same meanings as definedabove.)

According to the reaction scheme (2), a compound of the formula 3b! isreacted with a compound of the formula 2a! to give a compound of formula5! and if necessary, this compound is deprotected to produce a compoundof the formula 1! wherein R¹ is a hydrogen atom.

The reaction may be conducted under the same conditions as those for thereaction scheme (1). The conditions for the deprotection are the same asthose defined above.

The molar ratio of the starting compounds may be defined freely.Usually, the compound of the formula 3b! may be reacted with thecompound of the formula 2a! in an amount of from 0.8 to 1.5 times by molthe latter. ##STR7## (In these formulae, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A,D, E, G, X, Y and Z have the same meanings as defined above; Vrepresents a halogen atom or a leaving group such as chlorine atom,bromine atom, iodine atom, a methanesulfonyloxy group, apara-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, etc.when R¹ is a hydrogen atom, an alkyl group, an alkenyl group, an alkynylgroup or an aralkyl group, while V represents a halogen atom such aschlorine atom, bromine atom, iodine atom, etc., or a methoxy group, anethoxy group, a methylthio group, an ethylthio group, etc. when R¹ is anacyl group.)

According to the reaction scheme (3), a compound of the formula 5! isreacted with a compound of the formula 4a! to give a compound of theformula 1a! and, if necessary, the obtained compound is deprotected toproduce a compound of the formula 1! wherein R¹ represents thesubstituents other than hydrogen atom. The reaction may be conductedunder the same conditions as those for the reaction scheme (1). Theconditions for the deprotection are the same as those defined above.##STR8## (In these formulae, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A, D, E, G, X,Y, Z and V have the same meanings as defined above.)

According to the reaction scheme (4), a compound of the formula 6! isreacted with a compound of the formula 3a! to give a compound of theformula 1a! and, if necessary, the obtained compound is deprotected toproduce a compound of the formula 1! wherein R¹ represents thesubstituents other than hydrogen atom. The reaction may be conductedunder the same conditions as those for the reaction scheme (1). Theconditions for the deprotection are the same as those defined above.##STR9## (In these formulae, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A, D, E, G, X,Y, Z and V have the same meanings as defined above.)

According to the reaction scheme (5), a compound of the formula 7! isreacted with a compound of the formula 2a! to give a compound of theformula 1a! and, if necessary, the obtained compound is deprotected toproduce a compound of the formula 1! wherein R¹ represents thesubstituents other than hydrogen atom. The reaction may be conductedunder the same conditions as those for the reaction scheme (1). Theconditions for the deprotection are the same as those defined above.##STR10## (In these formulae, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A, D, E, G, X,Y and Z have the same meanings as defined above.)

According to the reaction scheme (6), a compound of the formula 1b! isreacted with a base to thereby remove its 5-positioned hydrogen atomtherefrom, the resulting compound is then reacted with an electrophilicagent to produce a compound of the formula 1a!, and, if necessary, theobtained compound is deprotected to obtain a compound of the formula 1!.

Usually, the reaction may be conducted, using, as the base, a metalamide such as lithium diisopropylamide, lithium hexamethyldisilazide,lithium 2,2,6,6-tetramethylpiperidide, etc.; an alkali metal such aslithium, sodium, etc.; a metal hydride such as potassium hydride, etc.;or an alkyl metal such as methyl lithium, n-butyl lithium, etc.

As the electrophilic agent, usable are halogens such as fluorine,chlorine, bromine, iodine, etc.; alkyl halides such as1,1,2,2-tetrafluoro-1,2-dibromoethane, 1,2-dibromoethane, methyl iodide,propyl iodide, etc.; isocyanates such as methyl isocyanate, cyclohexylisocyanate, etc.; acid halides such as acetyl chloride, ethylchloroformate, etc.; amides such as N-methoxy-N-methylbenzoylamide,dimethylformamide, etc.; esters such as ethyl acetate, triethyl borate,etc.; carbon dioxide, etc.

The reaction conditions such as the reaction solvent, the reactiontemperature and the molar ratio of the starting compounds may be thesame as those for the reaction scheme (1). The conditions for thedeprotection are the same as those defined above. ##STR11## (In theseformulae, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A, D, E, G, X, Y and Z have thesame meanings as defined above; W represents a halogen atom such aschlorine, bromine, iodide, etc.)

According to the reaction scheme (7), a compound of the formula 1c! issubjected to halogen-metal exchanging reaction at its 5-positionedhalogen, using an organolithium reagent or an alkali metal, theresulting compound is then reacted with an electrophilic agent in theabsence or presence of a catalyst to synthesize a compound of theformula 1a!, and, if necessary, the obtained compound is deprotected toobtain a compound of the formula 1!.

Usually, the reaction may be conducted, using an organolithium reagentsuch as butyl lithium, methyl lithium, etc., or an alkali metal such aslithium, sodium, potassium, etc.

As the catalyst, if desired, usable are palladium catalysts such astetrakis(triphenylphosphine) palladium(0), palladium(II) chloride, etc.;nickel catalysts such as dichloro 1,3-bis(diphenylphosphine)propane!nickel(II), tetrakis (tri-p-tolylphosphite) nickel(0), etc.; rutheniumcatalysts such as dichloro-tris(triphenylphosphine) ruthenium, etc.; andrhodium catalysts such as chloro-tris(triphenylphosphine) rhodium, etc.

This reaction may be conducted under the same conditions as those forthe reaction scheme (6). The conditions for the deprotection are thesame as those defined above. ##STR12## (In these formulae, R¹, R², R³,R⁴, R⁵, R⁶, R⁷, A, D, E, G, X, Y, Z and V have the same meanings asdefined above.)

According to the reaction scheme (8), a compound of the formula 1d! isreacted with an organometallic reagent or an alkyne or alkene in theabsence or presence of a catalyst to synthesize a compound of theformula 1a!, and, if necessary, the obtained compound is deprotected toobtain a compound of the formula 1!.

As the organometallic reagent in this reaction, usable are organolithiumreagents such as methyl lithium, n-butyl lithium, phenyl lithium,4-methylphenyl lithium, etc.; organomagnesium reagents such as methylmagnesium bromide, phenyl magnesium bromide, etc.; organoaluminiumreagents such as diisobutyl-1-hexenyl aluminium, etc.; organozincreagents such as methyl zinc bromide, phenyl zinc bromide, etc.;organotin reagents such as trimethylvinyl tin, etc.; organoboronreagents such as 3-methylphenylboric acid, etc.; organocopper reagentssuch as methyl copper, phenyl copper, lithium methylcuprate, etc.; metalalkoxides such as sodium methoxide, sodium phenoxide, etc.; metalmercaptides such as sodium methylmercaptide, sodium phenylmercaptide,etc. Also usable are alkynes such as phenylacetylene,trimethylsilylacetylene, etc.; and alkenes such as acrolein,acrylonitrile, etc.

As the catalyst, if desired, usable are palladium catalysts such astetrakis(triphenylphosphine) palladium(0), palladium(II) chloride, etc.;nickel catalysts such as dichloro 1,3-bis(diphenylphosphine)propane!nickel(II), tetrakis (tri-p-tolylphosphite) nickel(0), etc.; rutheniumcatalysts such as dichloro-tris(triphenylphosphine) ruthenium, etc.; andrhodium catalysts such as chloro-tris(triphenylphosphine) rhodium, etc.

This reaction may be conducted under the same conditions as those forthe reaction scheme (6). The conditions for the deprotection are thesame as those defined above. ##STR13## (In these formulae, R¹, R², R³,R⁴, R⁵, R⁶, R⁷, A, D, E, G, X, Y, Z and V have the same meanings asdefined above; M represents a metal atom such as lithium, copper, etc.,a metal halide such as zinc chloride, magnesium bromide, etc., an alkylmetal such as trimethyl tin, tributyl tin, etc., or boric acid.)

According to the reaction scheme (9), a compound of the formula 1e! isreacted with an organic halide in the absence or presence of a catalystto synthesize a compound of the formula 1a!, and optionally this isdeprotected to obtain a compound of the formula 1!.

As the organic halide, usable are alkyl halides such as methyl iodide,propyl iodide, etc.; aryl halides such as phenyl iodide,2-bromobenzonitrile, etc.; alkene halides such as vinyl bromide, etc.

As the catalyst, if desired, usable are palladium catalysts such astetrakis(triphenylphosphine) palladium(0), palladium(II) chloride, etc.;nickel catalysts such as dichloro 1,3-bis(diphenylphosphine)propane!nickel(II), tetrakis (tri-p-tolylphosphite) nickel(0), etc.; rutheniumcatalysts such as dichloro-tris(triphenylphosphine) ruthenium, etc.; andrhodium catalysts such as chloro-tris(triphenylphosphine) rhodium, etc.

This reaction may be conducted under the same conditions as those forthe reaction scheme (6). The conditions for the deprotection are thesame as those defined above. ##STR14## (In these formulae, R¹, R², R³,R⁴, R⁵, R⁶, R⁷, A, D, E, G, X, Y, Z and V have the same meanings asdefined above.)

According to the reaction scheme (10), a compound of the formula 1f! isreacted with an alkyl halide or acid halide in the absence or presenceof a catalyst to produce a compound of the formula 1a!, and, ifnecessary, the obtained compound is deprotected to obtain a compound ofthe formula 1!.

This reaction may be normally conducted in the presence of an inorganicbase such as potassium carbonate, sodium carbonate, lithium carbonate,potassium hydrogencarbonate, sodium hydrogencarbonate, lithiumhydroxide, etc.

Apart from the above-mentioned inorganic bases, also employable aremetal hydrides such as sodium hydride, potassium hydride, n-butyllithium, etc.; metal alkoxides such as sodium methoxide, sodiumethoxide, potassium t-butoxide, etc.; metal amides such as sodium amide,lithium diisopropylamide, lithium hexamethyldisilazide, lithium2,2,6,6-tetramethylpiperidide, etc.; and organic bases such astrimethylamine, triethylamine, pyridine, diisopropylethylamine, etc.

To conduct this reaction, a quaternary ammonium halide such as Adogen464 methyltrialkyl(C₈₋₁₀) ammonium chloride; trade name by AshlandChemical Co.! or the like may be used as the catalyst, if desired. Thisreaction may be conducted under the same conditions as those for thereaction scheme (6). The conditions for the deprotection are the same asthose mentioned above. ##STR15## (In these formulae, R¹, R², R³, R⁴, R⁵,R⁶, R⁷, A, D, E, G, X, Y, Z and V have the same meanings as definedabove.)

According to the reaction scheme (11), a compound of the formula 1c! isreacted with a primary or secondary amine to give a compound of theformula 1a!, and, if necessary, the obtained compound is deprotected toproduce a compound of the formula 1!.

This reaction may be generally conducted in the presence of an inorganicbase such as potassium carbonate, sodium carbonate, lithium carbonate,potassium hydrogencarbonate, sodium hydrogencarbonate, lithiumhydroxide, etc.

As the catalyst for the reaction, if desired, usable are coppercatalysts such as copper, copper(I) oxide, copper(II) oxide, etc.,singly or as a combination of them.

As the amine, usable are alkylamines such as n-propylamine,n-butylamine, diethylamine, etc., and arylamines such as aniline, etc.

This reaction may be conducted under the same conditions as those forthe reaction scheme 1!. The conditions for the deprotection are the sameas those defined above.

Compounds of the formulae 6! and 7! which are used as the startingcompounds in the above-mentioned methods may be produced, for example,according to the methods defined below. ##STR16## (In these formulae,R¹, R⁴, R⁵, R⁶, R⁷, E, G, Y, Z and V have the same meanings as definedabove.)

According to the reaction scheme (12), a compound of the formula 2b! isreacted with a compound of the formula 4a! to synthesize a compound offormula 6!. This reaction may be conducted under the same conditions asthose for the reaction scheme (3). ##STR17## (In these formulae, R¹, R⁴,R⁵, R⁶, R⁷, E, G, Y, Z and V have the same meanings as defined above.)

According to the reaction scheme (13), a compound of the formula 4b! isreacted with a compound of the formula 2a! to synthesize a compound ofthe formula 6!. This reaction may be conducted under the same conditionsas those for the reaction scheme (1). ##STR18## (In these formulae, R¹,R², R³, A, D, X and V have the same meanings as defined above.)

According to the reaction scheme (14), a compound of the formula 3b! isreacted with a compound of the formula 4a! to synthesize a compound ofthe formula 7!. This reaction may be conducted under the same conditionsas those for the reaction scheme (2). ##STR19## (In these formulae, R¹,R², R³, A, D, X and V have the same meanings as defined above.)

According to the reaction scheme (15), a compound of the formula 4b! isreacted with a compound of the formula 3a! to synthesize a compound ofthe formula 7!. This reaction may be conducted under the same conditionsas those for the reaction scheme (1).

Next, methods for producing compounds of the formulae 3a! and 3b! whichare the starting compounds in the above-mention methods will beexplained below.

Of compounds of formula 3b!, those of formula 11! wherein X is anitrogen atom may be synthesized according to the methods described in,for example, Z. Chem., 8, 420 (1969); Aust. J. Chem., 36, 135 (1983);Org. Prep. Proded. Int., 17, 70 (1985); J. Heterocycl. Chem., 19, 1265(1982); J. Heterocycl. Chem., 19, 1267 (1982); J. Med. Chem., 7, 259(1964); J. Heterocycl. Chem., 17, 73 (1980); Monatsh. Chem., 112, 875(1981); Tetrahedron Lett., 2991 (1979); Chem. Ber., 98, 2576 (1965);Helv. Chim. Acta, 42, 763 (1959), etc. ##STR20## In these formulae, R²,R³, A, D and V have the same meanings as defined above; V¹ represents ahalogen atom (e.g., chlorine, bromine, etc.), a hydroxyl group, analkoxy group (e.g.,methoxy, ethoxy, etc.), or an amino group (e.g., NH₂,NMe₂, NHPh, etc.).!

Briefly, a compound of the formula 8! is reacted with a compound of theformula 9! or 10! to synthesize a compound of the formula 11!; oralternatively, a compound of the formula 11a! is reacted with a compoundof V-A-D in a homogeneous system or a two-layer system to synthesize thesame.

Of compounds of the formula 3b!, those of the formula 14! wherein X is anitrogen atom may be produced according to the methods described in, forexample, J. Amer. Chem. Soc., 78, 784 (1956); J, Org. Chem., 21, 1240(1956); EP-320765; J. Prakt. Chem., 331, 552 (1989); DD-248587; J.Heterocycl. Chem., 23, 1035 (1986); J. Heterocycl. Chem., 22, 1093(1985); Synthesis, 794 (1985); Synthesis, 3, 276 (1984); EP-53698;EP-53699; EP-53678; Chem. Ber., 114, 2834 (1981); DD-149517; J. Gen.Chem., USSR 50, 2116 (1980); J. Heterocycl. Chem, 17, 1527 (1980); J.Heterocycl. Chem., 11, 423 (1974); J. Chem. Soc., C 1501 (1971); J.Chem. Soc., C 1610 (1971); Helv. Chim. Acta, 36, 86 (1956); Liebigs Ann.Chem., 339, 117 (1905), etc. ##STR21## (In these formulae, R², R³, A, Dand V have the same meanings as defined above.)

Briefly, a compound of the formula 12! is reacted with hydrazine tosynthesize a compound of the formula 14!, or alternatively, a compoundof the formula 13! is reacted with ammonia to synthesize the same.

Of compounds of the formula 3a!, those of formula 17! wherein X is anitrogen atom may be produced according to the methods described in, forexample, J. Chem. Soc C 1507 (1968); J. Org. Chem., 25, 1259 (1960); J.Amer. Chem. Soc., 73, 4664 (1951); Gazz. Chim. Ital., 78, 332 (1948);Liebigs Ann. Chem., 338, 183 (1905); Liebigs Ann. Chem., 338, 267(1905), etc. ##STR22## (In these formulae, R², R³, A, D and V have thesame meanings as defined above.)

Briefly, a compound of the formula 17! may be synthesized by reacting acompound of the formula 15! and a phosphorus oxyhalide, or reacting acompound of the formula 16! and a diazo compound, or diazoating acompound of the formula 11! followed by reacting the resulting diazocompound and a copper halide.

Of compounds of the formula 3a!, those of the formula 22! wherein X is anitrogen atom may be produced according to the methods described in, forexample, J. Chem. Soc., 2769 (1961); Bull. Chem. Soc. Jpn., 46, 1572(1973); J. Amer. Chem. Soc., 73, 4664 (1951); J. Amer. Chem. Soc., 76,3686 (1954); J. Heterocycl. Chem., 26, 241 (1989); Acta Chem. Scand.,33, 483 (1979); J. Org. Chem., 36, 2542 (1971); Bull. Soc. Chim. Fr.,1974 (1970); J. Chem. Soc. C 1507 (1968); J. Gen. Chem., USSR 30, 3251(1960); J. Pharm. Soc., Japan, 61, 26 (1941); J. Chem. Soc., 1739(1934); J. Chem. Soc., 475 (1933); Liebigs Ann. Chem., 338, 183 (1905);Chem. Ber., 33, 2595 (1900); J. Heterocycl. Chem., 28, 1545 (1991), etc.##STR23## (In these formulae, R², R³, A, D and V have the same meaningsas defined above.)

Briefly, a compound of the formula 22! may be synthesized by reacting acompound of the formula 18! and a phosphorus oxyhalide, or reacting acompound of the formula 19! and a halogen (e.g., chlorine, bromine), orreacting a compound of the formula 20! and a diazo compound, ordiazoating a compound of the formula 21! followed by reacting theresulting diazo compound and a copper halide.

Of compounds of the formula 3a!, those of the formula 24! wherein X is anitrogen atom may be produced according to the methods described in, forexample, J. Med. Chem., 32, 2573 (1989), etc. ##STR24## (In theseformulae, R², R³, A, D and V have the same meanings as defined above.)

Briefly, a compound of the formula 23! is reacted with an alkyl halidein the presence of an aqueous solution of Adogen 464, potassiumcarbonate or sodium hydroxide in toluene to synthesize a compound of theformula 24!.

As the routes for administering the pyrazole compounds of the formula 1!and their tautomers and salts of the present invention, they may beadministered parenterally as injection (subcutaneous, intravascular,intramuscular or intraabdominal injection), ointment, suppositories,aerosol, etc., or orally as tablets, capsules, granules, pills, syrup,solution, emulsion, suspension, etc.

The medicinal compositions of the present invention contain at least oneof the above-mentioned compounds of the formula 1! and their tautomersand salts in an amount of approximately from 0.1 to 99.5% by weight asthe compound of the formula 1!, preferably approximately from 0.5 to 95%by weight as the same, relative to the total weight of the composition.The compounds of the formula 1! and the compositions containing them maycontain other pharmacologically active compounds. The compositions maycontain a plurality of the compounds of the formula 1!.

The clinical dose of the compounds of the formula 1! to be administeredto patients varies, depending on the age, the body weight, thesensitivity and the condition of the patient. Usually, the effectivedose of the compound of the formula 1! for an adult is approximatelyfrom 0.003 to 1.5 g/day, preferably approximately from 0.01 to 0.6g/day. If desired, however, doses which are outside the defined rangemay also be employed.

The compounds of the formula 1! may be formulated into pharmaceuticalpreparations in accordance with conventional methods commonly employedfor the preparations of pharmaceutical formulations.

Namely, tablets, capsules, granules or pills for oral administration,may be prepared by using excipients such as white sugar, lactose,glucose, starch or mannitol; binders such as syrup, arabic gum, gelatin,sorbitol, tragacanth gum, methyl cellulose or polyvinylpyrrolidone;disintegrators such as starch, carboxymethyl cellulose or its calciumsalt, crystal cellulose powder or polyethylene glycol; lubricants suchas talc, magnesium or calcium stearate, silica; and smoothers such assodium laurate, glycerol, etc.

The injections, solutions, emulsions, suspensions, syrups and aerosolmay be prepared using a solvent for the active ingredient such as water,ethyl alcohol, isopropyl alcohol, propylene glycol, 1,3-butylene glycolor polyethylene glycol; surfactants such as sorbitan fatty acid esters,polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acidesters, polyoxyethylene ether of hydrogenated castor oil, lecithin;suspending agents such as cellulose derivatives such as sodiumcarboxymethyl cellulose and methyl cellulose or natural rubbers such astragacanth or arabic gum; preservatives such as para-hydroxybenzoates,benzalkonium chloride, salts of sorbic acid, etc. The suppositories maybe prepared by using, cacao butter, polyethylene glycol, lanolin,coconut oil, etc.

As examples of the compounds of the present invention, mentioned are thecompounds described in Tables 1 to 5 below and their pharmacologicallyacceptable salts, in addition to the compounds produced in the exampleswhich follow hereunder.

In the tables, "n-" means normal; "i-" means iso; "c-" means cyclo;"sec-" means secondary; "t-" means tertiary; "Me" means methyl; "Et"means ethyl; "Pr" means propyl; "Bu" means butyl; "Pen" means pentyl;"Hex" means hexyl; "Ph" means phenyl; and "Bz" means benzyl. In these,J¹ ═NHCOEt; J² ═N(n-Pen)COPh; U═COOH; and T means the followingsubstituent.

                  TABLE 1                                                         ______________________________________                                         ##STR25##                                                                     ##STR26##                                                                    R.sup.1  R.sup.2   R.sup.3       R.sup.7                                                                           A                                        ______________________________________                                        n-Pr     U         F             T   --                                       n-Pr     U         Cl            T   --                                       n-Pr     U         Br            T   --                                       n-Pr     U         I             T   --                                       n-Pr     U         Me            T   --                                       n-Pr     U         CF.sub.3      T   --                                       n-Pr     U         Et            T   --                                       n-Pr     U         n-Pr          T   --                                       n-Pr     U         NO.sub.2      T   --                                       n-Pr     U         NH.sub.2      T   --                                       n-Pr     U         NHCOPh        T   --                                       n-Pr     U         CHO           T   --                                       n-Pr     U         CN            T   --                                       n-Pr     U         Ph            T   --                                       n-Pr     U         F             T   CH.sub.2                                 n-Pr     U         Cl            T   CH.sub.2                                 n-Pr     U         Br            T   CH.sub.2                                 n-Pr     U         I             T   CH.sub.2                                 n-Pr     U         Me            T   CH.sub.2                                 n-Pr     U         CF.sub.3      T   CH.sub.2                                 n-Pr     U         Et            T   CH.sub.2                                 n-Pr     U         n-Pr          T   CH.sub.2                                 n-Pr     U         NO.sub.2      T   CH.sub.2                                 n-Pr     U         NH.sub.2      T   CH.sub.2                                 n-Pr     U         NHCOPh        T   CH.sub.2                                 n-Pr     U         CHO           T   CH.sub.2                                 n-Pr     U         CN            T   CH.sub.2                                 n-Pr     U         Ph            T   CH.sub.2                                 Et       U         F             T   CH.sub.2                                 Et       U         Cl            T   CH.sub.2                                 Et       U         Br            T   CH.sub.2                                 Et       U         I             T   CH.sub.2                                 Et       U         Me            T   CH.sub.2                                 Et       U         CF.sub.3      T   CH.sub.2                                 Et       U         Et            T   CH.sub.2                                 Et       U         n-Pr          T   CH.sub.2                                 Et       U         NO.sub.2      T   CH.sub.2                                 Et       U         NH.sub.2      T   CH.sub.2                                 Et       U         NHCOPh        T   CH.sub.2                                 Et       U         CHO           T   CH.sub.2                                 Et       U         CN            T   CH.sub.2                                 Et       U         Ph            T   CH.sub.2                                 n-Bu     U         F             T   CH.sub.2                                 n-Bu     U         Cl            T   CH.sub.2                                 n-Bu     U         Br            T   CH.sub.2                                 n-Bu     U         I             T   CH.sub.2                                 n-Bu     U         Me            T   CH.sub.2                                 n-Bu     U         CF.sub.3      T   CH.sub.2                                 n-Bu     U         Et            T   CH.sub.2                                 n-Bu     U         n-Pr          T   CH.sub.2                                 n-Bu     U         NO.sub.2      T   CH.sub.2                                 n-Bu     U         NH.sub.2      T   CH.sub.2                                 n-Bu     U         NHCOPh        T   CH.sub.2                                 n-Bu     U         CHO           T   CH.sub.2                                 n-Bu     U         CN            T   CH.sub.2                                 n-Bu     U         Ph            T   CH.sub.2                                 c-Pr     U         F             T   CH.sub.2                                 c-Pr     U         Cl            T   CH.sub.2                                 c-Pr     U         Br            T   CH.sub.2                                 c-Pr     U         I             T   CH.sub.2                                 c-Pr     U         Me            T   CH.sub.2                                 c-Pr     U         CF.sub.3      T   CH.sub.2                                 c-Pr     U         Et            T   CH.sub.2                                 c-Pr     U         n-Pr          T   CH.sub.2                                 c-Pr     U         NO.sub.2      T   CH.sub.2                                 c-Pr     U         NH.sub.2      T   CH.sub.2                                 c-Pr     U         NHCOPh        T   CH.sub.2                                 c-Pr     U         CHO           T   CH.sub.2                                 c-Pr     U         CN            T   CH.sub.2                                 c-Pr     U         Ph            T   CH.sub.2                                 n-Pr     U         F             T   (CH.sub.2).sub.3                         n-Pr     U         Cl            T   (CH.sub.2).sub.3                         n-Pr     U         Br            T   (CH.sub.2).sub.3                         n-Pr     U         I             T   (CH.sub.2).sub.3                         n-Pr     U         Me            T   (CH.sub.2).sub.3                         n-Pr     U         CF.sub.3      T   (CH.sub.2).sub.3                         n-Pr     U         Et            T   (CH.sub.2).sub.3                         n-Pr     U         n-Pr          T   (CH.sub.2).sub.3                         n-Pr     U         NO.sub.2      T   (CH.sub.2).sub.3                         n-Pr     U         NH.sub.2      T   (CH.sub.2).sub.3                         n-Pr     U         NHCOPh        T   (CH.sub.2).sub.3                         n-Pr     U         CHO           T   (CH.sub.2).sub.3                         n-Pr     U         CN            T   (CH.sub.2).sub.3                         n-Pr     U         Ph            T   (CH.sub.2).sub.3                         Et       U         F             T   (CH.sub.2).sub.3                         Et       U         Cl            T   (CH.sub.2).sub.3                         Et       U         Br            T   (CH.sub.2).sub.3                         Et       U         I             T   (CH.sub.2).sub.3                         Et       U         Me            T   (CH.sub.2).sub.3                         Et       U         CF.sub.3      T   (CH.sub.2).sub.3                         Et       U         Et            T   (CH.sub.2).sub.3                         Et       U         n-Pr          T   (CH.sub.2).sub.3                         Et       U         NO.sub.2      T   (CH.sub.2).sub.3                         Et       U         NH.sub.2      T   (CH.sub.2).sub.3                         Et       U         NHCOPh        T   (CH.sub.2).sub.3                         Et       U         CHO           T   (CH.sub.2).sub.3                         Et       U         CN            T   (CH.sub.2).sub.3                         Et       U         Ph            T   (CH.sub.2).sub.3                         n-Bu     U         F             T   (CH.sub.2).sub.3                         n-Bu     U         Cl            T   (CH.sub.2).sub.3                         n-Bu     U         Br            T   (CH.sub.2).sub.3                         n-Bu     U         I             T   (CH.sub.2).sub.3                         n-Bu     U         Me            T   (CH.sub.2).sub.3                         n-Bu     U         CF.sub.3      T   (CH.sub.2).sub.3                         n-Bu     U         Et            T   (CH.sub.2).sub.3                         n-Bu     U         n-Pr          T   (CH.sub.2).sub.3                         n-Bu     U         NO.sub.2      T   (CH.sub.2).sub.3                         n-Bu     U         NH.sub.2      T   (CH.sub.2).sub.3                         n-Bu     U         NHCOPh        T   (CH.sub.2).sub.3                         n-Bu     U         CHO           T   (CH.sub.2).sub.3                         n-Bu     U         CN            T   (CH.sub.2).sub.3                         n-Bu     U         Ph            T   (CH.sub.2).sub.3                         c-Pr     U         F             T   (CH.sub.2).sub.3                         c-Pr     U         Cl            T   (CH.sub.2).sub.3                         c-Pr     U         Br            T   (CH.sub.2).sub.3                         c-Pr     U         I             T   (CH.sub.2).sub.3                         c-Pr     U         Me            T   (CH.sub.2).sub.3                         c-Pr     U         CF.sub.3      T   (CH.sub.2).sub.3                         c-Pr     U         Et            T   (CH.sub.2).sub.3                         c-Pr     U         n-Pr          T   (CH.sub.2).sub.3                         c-Pr     U         NO.sub.2      T   (CH.sub.2).sub.3                         c-Pr     U         NH.sub.2      T   (CH.sub.2).sub.3                         c-Pr     U         NHCOPh        T   (CH.sub.2).sub.3                         c-Pr     U         CHO           T   (CH.sub.2).sub.3                         c-Pr     U         CN            T   (CH.sub.2).sub.3                         c-Pr     U         Ph            T   (CH.sub.2).sub.3                         n-Pr     U         F             T   (CH.sub.2).sub.4                         n-Pr     U         Cl            T   (CH.sub.2).sub.4                         n-Pr     U         Br            T   (CH.sub.2).sub.4                         n-Pr     U         I             T   (CH.sub.2).sub.4                         n-Pr     U         Me            T   (CH.sub.2).sub.4                         n-Pr     U         CF.sub.3      T   (CH.sub.2).sub.4                         n-Pr     U         Et            T   (CH.sub.2).sub.4                         n-Pr     U         n-Pr          T   (CH.sub.2).sub.4                         n-Pr     U         NO.sub.2      T   (CH.sub.2).sub.4                         n-Pr     U         NH.sub.2      T   (CH.sub.2).sub.4                         n-Pr     U         NHCOPh        T   (CH.sub.2).sub.4                         n-Pr     U         CHO           T   (CH.sub.2).sub.4                         n-Pr     U         CN            T   (CH.sub.2).sub.4                         n-Pr     U         Ph            T   (CH.sub.2).sub.4                         Et       U         F             T   (CH.sub.2).sub.4                         Et       U         Cl            T   (CH.sub.2).sub.4                         Et       U         Br            T   (CH.sub.2).sub.4                         Et       U         I             T   (CH.sub.2).sub.4                         Et       U         Me            T   (CH.sub.2).sub.4                         Et       U         CF.sub.3      T   (CH.sub.2).sub.4                         Et       U         Et            T   (CH.sub.2).sub.4                         Et       U         n-Pr          T   (CH.sub.2).sub.4                         Et       U         NO.sub.2      T   (CH.sub.2).sub.4                         Et       U         NH.sub.2      T   (CH.sub.2).sub.4                         Et       U         NHCOPh        T   (CH.sub.2).sub.4                         Et       U         CHO           T   (CH.sub.2).sub.4                         Et       U         CN            T   (CH.sub.2).sub.4                         Et       U         Ph            T   (CH.sub.2).sub.4                         n-Bu     U         F             T   (CH.sub.2).sub.4                         n-Bu     U         Cl            T   (CH.sub.2).sub.4                         n-Bu     U         Br            T   (CH.sub.2).sub.4                         n-Bu     U         I             T   (CH.sub.2).sub.4                         n-Bu     U         Me            T   (CH.sub.2).sub.4                         n-Bu     U         CF.sub.3      T   (CH.sub.2).sub.4                         n-Bu     U         Et            T   (CH.sub.2).sub.4                         n-Bu     U         n-Pr          T   (CH.sub.2).sub.4                         n-Bu     U         NO.sub.2      T   (CH.sub.2).sub.4                         n-Bu     U         NH.sub.2      T   (CH.sub.2).sub.4                         n-Bu     U         NHCOPh        T   (CH.sub.2).sub.4                         n-Bu     U         CHO           T   (CH.sub.2).sub.4                         n-Bu     U         CN            T   (CH.sub.2).sub.4                         n-Bu     U         Ph            T   (CH.sub.2).sub.4                         c-Pr     U         F             T   (CH.sub.2).sub.4                         c-Pr     U         Cl            T   (CH.sub.2).sub.4                         c-Pr     U         Br            T   (CH.sub.2).sub.4                         c-Pr     U         I             T   (CH.sub.2).sub.4                         c-Pr     U         Me            T   (CH.sub.2).sub.4                         c-Pr     U         CF.sub.3      T   (CH.sub.2).sub.4                         c-Pr     U         Et            T   (CH.sub.2).sub.4                         c-Pr     U         n-Pr          T   (CH.sub.2).sub.4                         c-Pr     U         NO.sub.2      T   (CH.sub.2).sub.4                         c-Pr     U         NH.sub.2      T   (CH.sub.2).sub.4                         c-Pr     U         NHCOPh        T   (CH.sub.2).sub.4                         c-Pr     U         CHO           T   (CH.sub.2).sub.4                         c-Pr     U         CN            T   (CH.sub.2).sub.4                         c-Pr     U         Ph            T   (CH.sub.2).sub.4                         n-Pr     U         F             T   C(O)                                     n-Pr     U         Cl            T   C(O)                                     n-Pr     U         Br            T   C(a)                                     n-Pr     U         I             T   C(O)                                     n-Pr     U         Me            T   C(O)                                     n-Pr     U         CF.sub.3      T   C(O)                                     n-Pr     U         Et            T   C(O)                                     n-Pr     U         n-Pr          T   C(O)                                     n-Pr     U         NO.sub.2      T   C(O)                                     n-Pr     U         NH.sub.2      T   C(O)                                     n-Pr     U         NHCOPh        T   C(O)                                     n-Pr     U         CHO           T   C(O)                                     n-Pr     U         CN            T   C(O)                                     n-Pr     U         Ph            T   C(O)                                     n-Pr     U         F             T   (CH.sub.2).sub.2 CO                      n-Pr     U         Cl            T   (CH.sub.2).sub.2 CO                      n-Pr     U         Br            T   (CH.sub.2).sub.2 CO                      n-Pr     U         I             T   (CH.sub.2).sub.2 CO                      n-Pr     U         Me            T   (CH.sub.2).sub.2 CO                      n-Pr     U         CF.sub.3      T   (CH.sub.2).sub.2 CO                      n-Pr     U         Et            T   (CH.sub.2).sub.2 CO                      n-Pr     U         n-Pr          T   (CH.sub.2).sub.2 CO                      n-Pr     U         NO.sub.2      T   (CH.sub.2).sub.2 CO                      n-Pr     U         NH.sub.2      T   (CH.sub.2).sub.2 CO                      n-Pr     U         NHCOPh        T   (CH.sub.2).sub.2 CO                      n-Pr     U         CHO           T   (CH.sub.2).sub.2 CO                      n-Pr     U         CN            T   (CH.sub.2).sub.2 CO                      n-Pr     U         Ph            T   (CH.sub.2).sub.2 CO                      Et       U         F             T   (CH.sub.2).sub.2 CO                      Et       U         Cl            T   (CH.sub.2).sub.2 CO                      Et       U         Br            T   (CH.sub.2).sub.2 CO                      Et       U         I             T   (CH.sub.2).sub.2 CO                      Et       U         Me            T   (CH.sub.2).sub.2 CO                      Et       U         CF.sub.3      T   (CH.sub.2).sub.2 CO                      Et       U         Et            T   (CH.sub.2).sub.2 CO                      Et       U         n-Pr          T   (CH.sub.2).sub.2 CO                      Et       U         NO.sub.2      T   (CH.sub.2).sub.2 CO                      Et       U         NH.sub.2      T   (CH.sub.2).sub.2 CO                      Et       U         NHCOPh        T   (CH.sub.2).sub.2 CO                      Et       U         CHO           T   (CH.sub.2).sub.2 CO                      Et       U         CN            T   (CH.sub.2).sub.2 CO                      Et       U         Ph            T   (CH.sub.2).sub.2 CO                      n-Bu     U         F             T   (CH.sub.2).sub.2 CO                      n-Bu     U         Cl            T   (CH.sub.2).sub.2 CO                      n-Bu     U         Br            T   (CH.sub.2).sub.2 CO                      n-Bu     U         I             T   (CH.sub.2).sub.2 CO                      n-Bu     U         Me            T   (CH.sub.2).sub.2 CO                      n-Bu     U         CF.sub.3      T   (CH.sub.2).sub.2 CO                      n-Bu     U         Et            T   (CH.sub.2).sub.2 CO                      n-Bu     U         n-Pr          T   (CH.sub.2).sub.2 CO                      n-Bu     U         NO.sub.2      T   (CH.sub.2).sub.2 CO                      n-Bu     U         NH.sub.2      T   (CH.sub.2).sub.2 CO                      n-Bu     U         NHCOPh        T   (CH.sub.2).sub.2 CO                      n-Bu     U         CHO           T   (CH.sub.2).sub.2 CO                      n-Bu     U         CN            T   (CH.sub.2).sub.2 CO                      n-Bu     U         Ph            T   (CH.sub.2).sub.2 CO                      c-Pr     U         F             T   (CH.sub.2).sub.2 CO                      c-Pr     U         Cl            T   (CH.sub.2).sub.2 CO                      c-Pr     U         Br            T   (CH.sub.2).sub.2 CO                      c-Pr     U         I             T   (CH.sub.2).sub.2 CO                      c-Pr     U         Me            T   (CH.sub.2).sub.2 CO                      c-Pr     U         CF.sub.3      T   (CH.sub.2).sub.2 CO                      c-Pr     U         Et            T   (CH.sub.2).sub.2 CO                      c-Pr     U         n-Pr          T   (CH.sub.2).sub.2 CO                      c-Pr     U         NO.sub.2      T   (CH.sub.2).sub.2 CO                      c-Pr     U         NH.sub.2      T   (CH.sub.2).sub.2 CO                      c-Pr     U         NHCOPh        T   (CH.sub.2).sub.2 CO                      c-Pr     U         CHO           T   (CH.sub.2).sub.2 CO                      c-Pr     U         CN            T   (CH.sub.2).sub.2 CO                      c-Pr     U         Ph            T   (CH.sub.2).sub.2 CO                      n-Pr     U         F             T   CH.sub.2 COCH.sub.2                      n-Pr     U         Cl            T   CH.sub.2 COCH.sub.2                      n-Pr     U         Br            T   CH.sub.2 COCH.sub.2                      n-Pr     U         I             T   CH.sub.2 COCH.sub.2                      n-Pr     U         Me            T   CH.sub.2 COCH.sub.2                      n-Pr     U         CF.sub.3      T   CH.sub.2 COCH.sub.2                      n-Pr     U         Et            T   CH.sub.2 COCH.sub.2                      n-Pr     U         n-Pr          T   CH.sub.2 COCH.sub.2                      n-Pr     U         NO.sub.2      T   CH.sub.2 COCH.sub.2                      n-Pr     U         NH.sub.2      T   CH.sub.2 COCH.sub.2                      n-Pr     U         NHCOPh        T   CH.sub.2 COCH.sub.2                      n-Pr     U         CHO           T   CH.sub.2 COCH.sub.2                      n-Pr     U         CN            T   CH.sub.2 COCH.sub.2                      n-Pr     U         Ph            T   CH.sub.2 COCH.sub.2                      Et       U         F             T   CH.sub.2 COCH.sub.2                      Et       U         Cl            T   CH.sub.2 COCH.sub.2                      Et       U         Br            T   CH.sub.2 COCH.sub.2                      Et       U         I             T   CH.sub.2 COCH.sub.2                      Et       U         Me            T   CH.sub.2 COCH.sub.2                      Et       U         CF.sub.3      T   CH.sub.2 COCH.sub.2                      Et       U         Et            T   CH.sub.2 COCH.sub.2                      Et       U         n-Pr          T   CH.sub.2 COCH.sub.2                      Et       U         NO.sub.2      T   CH.sub.2 COCH.sub.2                      Et       U         NH.sub.2      T   CH.sub.2 COCH.sub.2                      Et       U         NHCOPh        T   CH.sub.2 COCH.sub.2                      Et       U         CHO           T   CH.sub.2 COCH.sub.2                      Et       U         CN            T   CH.sub.2 COCH.sub.2                      Et       U         Ph            T   CH.sub.2 COCH.sub.2                      n-Bu     U         F             T   CH.sub.2 COCH.sub.2                      n-Bu     U         Cl            T   CH.sub.2 COCH.sub.2                      n-Bu     U         Br            T   CH.sub.2 COCH.sub.2                      n-Bu     U         I             T   CH.sub.2 COCH.sub.2                      n-Bu     U         Me            T   CH.sub.2 COCH.sub.2                      n-Bu     U         CF.sub.3      T   CH.sub.2 COCH.sub.2                      n-Bu     U         Et            T   CH.sub.2 COCH.sub.2                      n-Bu     U         n-Pr          T   CH.sub.2 COCH.sub.2                      n-Bu     U         NO.sub.2      T   CH.sub.2 COCH.sub.2                      n-Bu     U         NH.sub.2      T   CH.sub.2 COCH.sub.2                      n-Bu     U         NHCOPh        T   CH.sub.2 COCH.sub.2                      n-Bu     U         CHO           T   CH.sub.2 COCH.sub.2                      n-Bu     U         CN            T   CH.sub.2 COCH.sub.2                      n-Bu     U         Ph            T   CH.sub.2 COCH.sub.2                      c-Pr     U         F             T   CH.sub.2 COCH.sub.2                      c-Pr     U         Cl            T   CH.sub.2 COCH.sub.2                      c-Pr     U         Br            T   CH.sub.2 COCH.sub.2                      c-Pr     U         I             T   CH.sub.2 COCH.sub.2                      c-Pr     U         Me            T   CH.sub.2 COCH.sub.2                      c-Pr     U         CF.sub.3      T   CH.sub.2 COCH.sub.2                      c-Pr     U         Et            T   CH.sub.2 COCH.sub.2                      c-Pr     U         n-Pr          T   CH.sub.2 COCH.sub.2                      c-Pr     U         NO.sub.2      T   CH.sub.2 COCH.sub.2                      c-Pr     U         NH.sub.2      T   CH.sub.2 COCH.sub.2                      c-Pr     U         NHCOPh        T   CH.sub.2 COCH.sub.2                      c-Pr     U         CHO           T   CH.sub.2 COCH.sub.2                      c-Pr     U         CN            T   CH.sub.2 COCH.sub.2                      c-Pr     U         Ph            T   CH.sub.2 COCH.sub.2                      n-Pr     U         F             T   CH.sub.2 CH(Ph)                          n-Pr     U         Cl            T   CH.sub.2 CH(Ph)                          n-Pr     U         Br            T   CH.sub.2 CH(Ph)                          n-Pr     U         I             T   CH.sub.2 CH(Ph)                          n-Pr     U         Me            T   CH.sub.2 CH(Ph)                          n-Pr     U         CF.sub.3      T   CH.sub.2 CH(Ph)                          n-Pr     U         Et            T   CH.sub.2 CH(Ph)                          n-Pr     U         n-Pr          T   CH.sub.2 CH(Ph)                          n-Pr     U         c-Pr          T   CH.sub.2 CH(Ph)                          n-Pr     U         NO.sub.2      T   CH.sub.2 CH(Ph)                          n-Pr     U         NH.sub.2      T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)H        T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me).sub.2   T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)n-Bu     T   CH.sub.2 CH(Ph)                          n-Pr     U         N(nPen)H      T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCOPh        T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)CO-c-Hex T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCONHMe      T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)CONHPh   T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCONH-c-Hex  T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCOBz        T   CH.sub.2 CH(Ph)                          n-Pr     U         J.sub.1       T   CH.sub.2 CH(Ph)                          n-Pr     U         NBzCOO-n-Bu   T   CH.sub.2 CH(Ph)                          n-Pr     U         NBzCOO-i-Bu   T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCO-n-Bu     T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCOO-i-Bu    T   CH.sub.2 CH(Ph)                          n-Pr     U         NHCOCF.sub.3  T   CH.sub.2 CH(Ph)                          n-Pr     U         NHSO.sub.2 CF.sub.3                                                                         T   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)Ph       T   CH.sub.2 CH(Ph)                          n-Pr     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 CH(Ph)                          n-Pr     U         C(NH)NH.sub.2 T   CH.sub.2 CH(Ph)                          n-Pr     U         CHO           T   CH.sub.2 CH(Ph)                          n-Pr     U         CN            T   CH.sub.2 CH(Ph)                          n-Pr     U         U             T   CH.sub.2 CH(Ph)                          n-Pr     U         COOMe         T   CH.sub.2 CH(Ph)                          n-Pr     U         CONH.sub.2    T   CH.sub.2 CH(Ph)                          n-Pr     U         CONHCOMe      T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 NH.sub.2                                                                           T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 OH   T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 NHCOPh                                                                             T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 N(nPen)COPh                                                                        T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 NHCONHMe                                                                           T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 CONHPh                                                                             T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 COOH T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph            T   CH.sub.2 CH(Ph)                          n-Pr     U         Bz            T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 CH.sub.2 Ph                                                                        T   CH.sub.2 CH(Ph)                          n-Pr     U         2-thienyl     T   CH.sub.2 CH(Ph)                          n-Pr     U         3-furyl       T   CH.sub.2 CH(Ph)                          n-Pr     U         1-pyrrolyl    T   CH.sub.2 CH(Ph)                          n-Pr     U         1-imidazolyl  T   CH.sub.2 CH(Ph)                          n-Pr     U         1-pyrazolyl   T   CH.sub.2 CH(Ph)                          n-Pr     U         2-pyridyl     T   CH.sub.2 CH(Ph)                          n-Pr     U         1-pyrrolidinyl                                                                              T   CH.sub.2 CH(Ph)                          n-Pr     U         1-piperidyl   T   CH.sub.2 CH(Ph)                          n-Pr     U         1-piperazinyl T   CH.sub.2 CH(Ph)                          n-Pr     U         4-morpholinyl T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-Cl)      T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(3-Me)      T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(4-OMe)     T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-NO.sub.2)                                                                              T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(3-NH.sub.2)                                                                              T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(4-NMe.sub.2)                                                                             T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(4-J.sup.2) T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-Cl, 3-J.sup.1)                                                                         T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-Cl, 4-J.sup.1)                                                                         T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-Cl, 5-J.sup.1)                                                                         T   CH.sub.2 CH(Ph)                          n-Pr     U         Ph(2-Cl, 6-J.sup.1)                                                                         T   CH.sub.2 CH(Ph)                          n-Pr     U         CH.sub.2 CH.sub.2 Ph(2-Cl, 5-J.sup.1)                                                       T   CH.sub.2 CH(Ph)                          n-Pr     U         T             T   CH.sub.2 CH(Ph)                          Et       U         F             T   CH.sub.2 CH(Ph)                          Et       U         Cl            T   CH.sub.2 CH(Ph)                          Et       U         Br            T   CH.sub.2 CH(Ph)                          Et       U         I             T   CH.sub.2 CH(Ph)                          Et       U         Me            T   CH.sub.2 CH(Ph)                          Et       U         CF.sub.3      T   CH.sub.2 CH(Ph)                          Et       U         Et            T   CH.sub.2 CH(Ph)                          Et       U         n-Pr          T   CH.sub.2 CH(Ph)                          Et       U         c-Pr          T   CH.sub.2 CH(Ph)                          Et       U         NO.sub.2      T   CH.sub.2 CH(Ph)                          Et       U         NH.sub.2      T   CH.sub.2 CH(Rh)                          Et       U         N(Me)H        T   CH.sub.2 CH(Ph)                          Et       U         N(Me).sub.2   T   CH.sub.2 CH(Ph)                          Et       U         N(Me)n-Bu     T   CH.sub.2 CH(Ph)                          Et       U         N(nPen)H      T   CH.sub.2 CH(Ph)                          Et       U         NHCOPh        T   CH.sub.2 CH(Ph)                          Et       U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 CH(Ph)                          Et       U         C(NH)NH.sub.2 T   CH.sub.2 CH(Ph)                          Et       U         CHO           T   CH.sub.2 CH(Ph)                          Et       U         CN            T   CH.sub.2 CH(Ph)                          Et       U         U             T   CH.sub.2 CH(Ph)                          Et       U         COOMe         T   CH.sub.2 CH(Ph)                          Et       U         CONH.sub.2    T   CH.sub.2 CH(Ph)                          Et       U         CONHCOMe      T   CH.sub.2 CH(Ph)                          n-Bu     U         F             T   CH.sub.2 CH(Ph)                          n-Bu     U         Cl            T   CH.sub.2 CH(Ph)                          n-Bu     U         Br            T   CH.sub.2 CH(Ph)                          n-Bu     U         I             T   CH.sub.2 CH(Ph)                          n-Bu     U         Me            T   CH.sub.2 CH(Ph)                          n-Bu     U         CF.sub.3      T   CH.sub.2 CH(Ph)                          n-Bu     U         Et            T   CH.sub.2 CH(Ph)                          n-Bu     U         n-Pr          T   CH.sub.2 CH(Ph)                          n-Bu     U         c-Pr          T   CH.sub.2 CH(Ph)                          n-Bu     U         NO.sub.2      T   CH.sub.2 CH(Ph)                          n-Bu     U         NH.sub.2      T   CH.sub.2 CH(Ph)                          n-Bu     U         N(Me)H        T   CH.sub.2 CH(Ph)                          n-Bu     U         N(Me).sub.2   T   CH.sub.2 CH(Ph)                          n-Bu     U         N(Me)n-Bu     T   CH.sub.2 CH(Ph)                          n-Bu     U         N(nPen)H      T   CH.sub.2 CH(Ph)                          n-Bu     U         NHCOPh        T   CH.sub.2 CH(Ph)                          n-Bu     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 CH(Ph)                          n-Bu     U         C(NH)NH.sub.2 T   CH.sub.2 CH(Ph)                          n-Bu     U         CHO           T   CH.sub.2 CH(Ph)                          n-Bu     U         CN            T   CH.sub.2 CH(Ph)                          n-Bu     U         U             T   CH.sub.2 CH(Ph)                          n-Bu     U         COOMe         T   CH.sub.2 CH(Ph)                          n-Bu     U         CONH.sub.2    T   CH.sub.2 CH(Ph)                          n-Bu     U         CONHCOMe      T   CH.sub.2 CH(Ph)                          c-Pr     U         F             T   CH.sub.2 CH(Ph)                          c-Pr     U         Cl            T   CH.sub.2 CH(Ph)                          c-Pr     U         Br            T   CH.sub.2 CH(Ph)                          c-Pr     U         I             T   CH.sub.2 CH(Ph)                          c-Pr     U         Me            T   CH.sub.2 CH(Ph)                          c-Pr     U         CF.sub.3      T   CH.sub.2 CH(Ph)                          c-Pr     U         Et            T   CH.sub.2 CH(Ph)                          c-Pr     U         n-Pr          T   CH.sub.2 CH(Ph)                          c-Pr     U         c-Pr          T   CH.sub.2 CH(Ph)                          c-Pr     U         NO.sub.2      T   CH.sub.2 CH(Ph)                          c-Pr     U         NH.sub.2      T   CH.sub.2 CH(Ph)                          c-Pr     U         N(Me)H        T   CH.sub.2 CH(Ph)                          c-Pr     U         N(Me).sub.2   T   CH.sub.2 CH(Ph)                          c-Pr     U         N(Me)n-Bu     T   CH.sub.2 CH(Ph)                          c-Pr     U         N(nPen)H      T   CH.sub.2 CH(Ph)                          c-Pr     U         NHCOPh        T   CH.sub.2 CH(Ph)                          c-Pr     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 CH(Ph)                          c-Pr     U         C(NH)NH.sub.2 T   CH.sub.2 CH(Ph)                          c-Pr     U         CHO           T   CH.sub.3 CH(Ph)                          c-Pr     U         CN            T   CH.sub.2 CH(Ph)                          c-Pr     U         U             T   CH.sub.2 CH(Ph)                          c-Pr     U         COOMe         T   CH.sub.2 CH(Ph)                          c-Pr     U         CONH.sub.2    T   CH.sub.2 CH(Ph)                          c-Pr     U         CONHCOMe      T   CH.sub.2 CH(Ph)                          n-Pr     U         F             U   CH.sub.2 CH(Ph)                          n-Pr     U         Cl            U   CH.sub.2 CH(Ph)                          n-Pr     U         Br            U   CH.sub.2 CH(Ph)                          n-Pr     U         I             U   CH.sub.2 CH(Ph)                          n-Pr     U         Me            U   CH.sub.2 CH(Ph)                          n-Pr     U         CF.sub.3      U   CH.sub.2 CH(Ph)                          n-Pr     U         Et            U   CH.sub.2 CH(Ph)                          n-Pr     U         n-Pr          U   CH.sub.2 CH(Ph)                          n-Pr     U         c-Pr          U   CH.sub.2 CH(Ph)                          n-Pr     U         NO.sub.2      U   CH.sub.2 CH(Ph)                          n-Pr     U         NH.sub.2      U   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)H        U   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me).sub.2   U   CH.sub.2 CH(Ph)                          n-Pr     U         N(Me)n-Bu     U   CH.sub.2 CH (Ph)                         n-Pr     U         N(nPen)H      U   CH.sub.2 CH (Ph)                         n-Pr     U         NHCOPh        U   CH.sub.2 CH(Ph)                          n-Pr     U         NHC(NH)NH.sub.2                                                                             U   CH.sub.2 CH(Ph)                          n-Pr     U         C(NH)NH.sub.2 U   CH.sub.2 CH(Ph)                          n-Pr     U         CHO           U   CH.sub.2 CH(Ph)                          n-Pr     U         CN            U   CH.sub.2 CH(Ph)                          n-Pr     U         U             U   CH.sub.2 CH(Ph)                          n-Pr     U         COOMe         U   CH.sub.2 CH(Ph)                          n-Pr     U         CONH.sub.2    U   CH.sub.2 CH(Ph)                          n-Pr     U         CONHCOMe      U   CH.sub.2 CH(Ph)                          n-Pr     U         F             T   CH.sub.2 C(O)                            n-Pr     U         Cl            T   CH.sub.2 C(O)                            n-Pr     U         Br            T   CH.sub.2C(O)                             n-Pr     U         I             T   CH.sub.2C(O)                             n-Pr     U         Me            T   CH.sub.2C(O)                             n-Pr     U         CF.sub.3      T   CH.sub.2 C(O)                            n-Pr     U         Et            T   CH.sub.2 C(O)                            n-Pr     U         n-Pr          T   CH.sub.2 C(O)                            n-Pr     U         c-Pr          T   CH.sub.2 C(O)                            n-Pr     U         NO.sub.2      T   CH.sub.2 C(O)                            n-Pr     U         NH.sub.2      T   CH.sub.2 C(O)                            n-Pr     U         N(Me)H        T   CH.sub.2 C(O)                            n-Pr     U         N(Me).sub.2   T   CH.sub.2 C(O)                            n-Pr     U         N(Me)n-Bu     T   CH.sub.2 C(O)                            n-Pr     U         N(nPen)H      T   CH.sub.2 C(O)                            n-Pr     U         NHCOPh        T   CH.sub.2 C(O)                            n-Pr     U         N(Me)CO-c-Hex T   CH.sub.2 C(O)                            n-Pr     U         NHCONHMe      T   CH.sub.2 C(O)                            n-Pr     U         N(Me)CONHPh   T   CH.sub.2 C(O)                            n-Pr     U         NHCONH-c-Hex  T   CH.sub.2 C(O)                            n-Pr     U         NHCOBz        T   CH.sub.2 C(O)                            n-Pr     U         J.sup.1       T   CH.sub.2 C(O)                            n-Pr     U         NBzCO-n-Bu    T   CH.sub.2 C(O)                            n-Pr     U         NBzCOO-i-Bu   T   CH.sub.2 C(O)                            n-Pr     U         NHCO-n-Bu     T   CH.sub.2 C(O)                            n-Pr     U         NHCOO-i-Bu    T   CH.sub.2 C(O)                            n-Pr     U         NHCOCF.sub.3  T   CH.sub.2 C(O)                            n-Pr     U         NHSO.sub.2 CF.sub.3                                                                         T   CH.sub.2 C(O)                            n-Pr     U         N(Me)Ph       T   CH.sub.2 C(O)                            n-Pr     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 C(O)                            n-Pr     U         C(NH)NH.sub.2 T   CH.sub.2 C(O)                            n-Pr     U         CHO           T   CH.sub.2 C(O)                            n-Pr     U         CN            T   CH.sub.2 C(O)                            n-Pr     U         U             T   CH.sub.2 C(O)                            n-Pr     U         COOMe         T   CH.sub.2 C(O)                            n-Pr     U         CONH.sub.2    T   CH.sub.2 C(O)                            n-Pr     U         CONHCOMe      T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 NH.sub.2                                                                           T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2OH    T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 NHCOPh                                                                             T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 N(nPen)COPh                                                                        T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 NHCONHMe                                                                           T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 CONHPh                                                                             T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 COOH T   CH.sub.2 C(O)                            n-Pr     U         Ph            T   CH.sub.2 C(O)                            n-Pr     U         Bz            T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 CH.sub.2 Ph                                                                        T   CH.sub.2 C(O)                            n-Pr     U         2-thienyl     T   CH.sub.2 C(O)                            n-Pr     U         3-furyl       T   CH.sub.2 C(O)                            n-Pr     U         1-pyrrolyl    T   CH.sub.2 C(O)                            n-Pr     U         1-imidazolyl  T   CH.sub.2 C(O)                            n-Pr     U         1-pyrazolyl   T   CH.sub.2 C(O)                            n-Pr     U         2-pyridyl     T   CH.sub.2 C(O)                            n-Pr     U         1-pyrrolidinyl                                                                              T   CH.sub.2 C(O)                            n-Pr     U         1-piperidyl   T   CH.sub.2 C(O)                            n-Pr     U         1-piperazinyl T   CH.sub.2 C(O)                            n-Pr     U         4-morpholinyl T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-Cl)      T   CH.sub.2 C(O)                            n-Pr     U         Ph(3-Me)      T   CH.sub.2 C(O)                            n-Pr     U         Ph(4-OMe)     T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-NO.sub.2)                                                                              T   CH.sub.2 C(O)                            n-Pr     U         Ph(3-NH.sub.2)                                                                              T   CH.sub.2 C(O)                            n-Pr     U         Ph(4-NMe.sub.2)                                                                             T   CH.sub.2 C(O)                            n-Pr     U         Ph(4-J.sup.2) T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-Cl, 3-J.sup.1)                                                                         T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-Cl, 4-J.sup.1)                                                                         T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-Cl, 5-J.sup.1)                                                                         T   CH.sub.2 C(O)                            n-Pr     U         Ph(2-Cl, 6-J.sup.1)                                                                         T   CH.sub.2 C(O)                            n-Pr     U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   CH.sub.2 C(O)                            n-Pr     U         T             T   CH.sub.2 C(O)                            Et       U         F             T   CH.sub.2 C(O)                            Et       U         Cl            T   CH.sub.2 C(O)                            Et       U         Br            T   CH.sub.2 C(O)                            Et       U         I             T   CH.sub.2 C(O)                            Et       U         Me            T   CH.sub.2 C(O))                           Et       U         CF.sub.3      T   CH.sub.2 C(O)                            Et       U         Et            T   CH.sub.2 C(O)                            Et       U         n-Pr          T   CH.sub.2 C(O)                            Et       U         c-Pr          T   CH.sub.2 C(O)                            Et       U         NO.sub.2      T   CH.sub.2 C(O)                            Et       U         NH.sub.2      T   CH.sub.2 C(O)                            Et       U         N(Me)H        T   CH.sub.2 C(O)                            Et       U         N(Me).sub.2   T   CH.sub.2 C(O)                            Et       U         N(Me)n-Bu     T   CH.sub.2 C(O)                            Et       U         N(nPen)H      T   CH.sub.2 C(O)                            Et       U         NHCOPh        T   CH.sub.2 C(O)                            Et       U         N(Me)CO-c-Hex T   CH.sub.2 C(O)                            Et       U         NHCONHMe      T   CH.sub.2 C(O)                            Et       U         N(Me)CONHPh   T   CH.sub.2 C(O)                            Et       U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 C(O)                            Et       U         C(NH)NH.sub.2 T   CH.sub.2 C(O)                            Et       U         CHO           T   CH.sub.2 C(O)                            Et       U         CN            T   CH.sub.2 C(O)                            Et       U         U             T   CH.sub.2 C(O)                            Et       U         COOMe         T   CH.sub.2 C(O)                            Et       U         CONH.sub.2    T   CH.sub.2 C(O)                            Et       U         CONHCOMe      T   CH.sub.2 C(O)                            n-Bu     U         F             T   CH.sub.2 CO)                             n-Bu     U         Cl            T   CH.sub.2 C(O)                            n-Bu     U         Br            T   CH.sub.2 C(O)                            n-Bu     U         I             T   CH.sub.2 C(O)                            n-Bu     U         Me            T   CH.sub.2 C(O)                            n-Bu     U         CF.sub.3      T   CH.sub.2 C(O)                            n-Bu     U         Et            T   CH.sub.2 C(O)                            n-Bu     U         n-Pr          T   CH.sub.2 C(O)                            n-Bu     U         c-Pr          T   CH.sub.2 C(O)                            n-Bu     U         NO.sub.2      T   CH.sub.2 C(O)                            n-Bu     U         NH.sub.2      T   CH.sub.2 C(O)                            n-Bu     U         N(Me)H        T   CH.sub.2 C(O)                            n-Bu     U         N(Me).sub.2   T   CH.sub.2 C(O)                            n-Bu     U         N(Me)n-Bu     T   CH.sub.2 C(O)                            n-Bu     U         N(nPen)H      T   CH.sub.2C.(O)                            n-Bu     U         NHCOPh        T   CH.sub.2 C(O)                            n-Bu     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 C(O)                            n-Bu     U         C(NH)NH.sub.2 T   CH.sub.2 C(O)                            n-Bu     U         CHO           T   CH.sub.2 C(O)                            n-Bu     U         CN            T   CH.sub.2 C(O)                            n-Bu     U         U             T   CH.sub.2 C(O)                            n-Bu     U         COOMe         T   CH.sub.2 C(O)                            n-Bu     U         CONH.sub.2    T   CH.sub.2 C(O)                            n-Bu     U         CONHCHOMe     T   CH.sub.2 C(O)                            c-Pr     U         F             T   CH.sub.2 C(O)                            c-Pr     U         Cl            T   CH.sub.2 C(O)                            c-Pr     U         Br            T   CH.sub.2 C(O)                            c-Pr     U         I             T   CH.sub.2 C(O)                            c-Pr     U         Me            T   CH.sub.2 C(O)                            c-Pr     U         CF.sub.3      T   CH.sub.2 C(O)                            c-Pr     U         Et            T   CH.sub.2 C(O)                            c-Pr     U         n-Pr          T   CH.sub.2 C(O)                            c-Pr     U         c-Pr          T   CH.sub.2 C(O)                            c-Pr     U         NO.sub.2      T   CH.sub.2 C(O)                            c-Pr     U         NH.sub.2      T   CH.sub.2 C(O)                            c-Pr     U         N(Me)H        T   CH.sub.2 C(O)                            c-Pr     U         N(Me).sub.2   T   CH.sub.2 C(O)                            c-Pr     U         N(Me)n-Bu     T   CH.sub.2 C(O)                            c-Pr     U         N(nPen)H      T   CH.sub.2 C(O)                            c-Pr     U         NHCOPh        T   CH.sub.2 C(O)                            c-Pr     U         NHC(NH)NH.sub.2                                                                             T   CH.sub.2 C(O)                            c-Pr     U         C(NH)NH.sub.2 T   CH.sub.2 C(O)                            c-Pr     U         CHO           T   CH.sub.2 C(O)                            c-Pr     U         CN            T   CH.sub.2 C(O)                            c-Pr     U         U             T   CH.sub.2 C(O)                            c-Pr     U         COOMe         T   CH.sub.2 C(O)                            c-Pr     U         CONH.sub.2    T   CH.sub.2 C(O)                            c-Pr     U         CONHCOMe      T   CH.sub.2 C(O)                            n-Pr     U         F             T   (CH.sub.2).sub.2                         n-Pr     U         Cl            T   (CH.sub.2).sub.2                         n-Pr     U         Br            T   (CH.sub.2).sub.2                         n-Pr     U         I             T   (CH.sub.2).sub.2                         n-Pr     U         Me            T   (CH.sub.2).sub.2                         n-Pr     U         CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     U         Et            T   (CH.sub.2).sub.2                         n-Pr     U         n-Pr          T   (CH.sub.2).sub.2                         n-Pr     U         c-Pr          T   (CH.sub.2).sub.2                         n-Pr     U         NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     U         NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     U         N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     U         N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     U         N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     U         NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         n-Pr     U         NHCONHMe      T   (CH.sub.2).sub.2                         n-Pr     U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         n-Pr     U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         n-Pr     U         NHCOBz        T   (CH.sub.2).sub.2                         n-Pr     U         J.sup.1       T   (CH.sub.2).sub.2                         n-Pr     U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         n-Pr     U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         n-Pr     U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         n-Pr     U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         n-Pr     U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         n-Pr     U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         n-Pr     U         N(Me)Ph       T   (CH.sub.2).sub.2                         n-Pr     U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     U         CHO           T   (CH.sub.2).sub.2                         n-Pr     U         CN            T   (CH.sub.2).sub.2                         n-Pr     U         U             T   (CH.sub.2).sub.2                         n-Pr     U         COOMe         T   (CH.sub.2).sub.2                         n-Pr     U         CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     U         CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     U         Ph            T   (CH.sub.2).sub.2                         n-Pr     U         Bz            T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     U         2-thienyl     T   (CH.sub.2).sub.2                         n-Pr     U         3-furyl       T   (CH.sub.2).sub.2                         n-Pr     U         1-pyrrolyl    T   (CH.sub.2).sub.2                         n-Pr     U         1-imidazolyl  T   (CH.sub.2).sub.2                         n-Pr     U         1-pyrazolyl   T   (CH.sub.2).sub.2                         n-Pr     U         2-pyridyl     T   (CH.sub.2).sub.2                         n-Pr     U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         n-Pr     U         1-piperidyl   T   (CH.sub.2).sub.2                         n-Pr     U         1-piperazinyl T   (CH.sub.2).sub.2                         n-Pr     U         4-morpholinyl T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-Me)      T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Pr     U         Ph(2-Cl, 6-J.sup.1)                                                                         T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              n-Pr     U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           n-Pr     U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         n-Pr     U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-CH.sub.2).sup.2 J.sup.2)                                                               T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         n-Pr     U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         n-Pr     U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         n-Pr     U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         n-Pr     U         OH            T   (CH.sub.2).sub.2                         n-Pr     U         OMe           T   (CH.sub.2).sub.2                         n-Pr     U         OPh           T   (CH.sub.2).sub.2                         n-Pr     U         SH            T   (CH.sub.3).sub.2                         n-Pr     U         SPh           T   (CH.sub.2).sub.2                         n-Pr     U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         n-Pr     U         S-n-Bu        T   (CH.sub.2).sub.2                         n-Pr     U         2-pyrazinyl   T   (CH.sub.2).sub.2                         n-Pr     U         2-pyrimidinyl T   (CH.sub.2).sub.2                         n-Pr     U         3-pyridyl     T   (CH.sub.2).sub.2                         n-Pr     U         4-pyridyl     T   (CH.sub.2).sub.2                         n-Pr     U         T             T   (CH.sub.2).sub.2                         Me       U         F             T   (CH.sub.2).sub.2                         Me       U         Cl            T   (CH.sub.2).sub.2                         Me       U         Br            T   (CH.sub.2).sub.2                         Me       U         I             T   (CH.sub.2).sub.2                         Me       U         Me            T   (CH.sub.2).sub.2                         Me       U         CF.sub.3      T   (CH.sub.2).sub.2                         Me       U         Et            T   (CH.sub.2).sub.2                         Me       U         n-Pr          T   (CH.sub.2).sub.2                         Me       U         c-Pr          T   (CH.sub.2).sub.2                         Me       U         NO.sub.2      T   (CH.sub.2).sub.2                         Me       U         NH.sub.2      T   (CH.sub.2).sub.2                         Me       U         N(Me)H        T   (CH.sub.2).sub.2                         Me       U         N(Me).sub.2   T   (CH.sub.2).sub.2                         Me       U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         Me       U         N(nPen)H      T   (CH.sub.2).sub.2                         Me       U         NHCOPh        T   (CH.sub.2).sub.2                         Me       U         J.sup.1       T   (CH.sub.2).sub.2                         Me       U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         Me       U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         Me       U         CHO           T   (CH.sub.2).sub.2                         Me       U         CN            T   (CH.sub.2).sub.2                         Me       U         U             T   (CH.sub.2).sub.2                         Me       U         COOMe         T   (CH.sub.3).sub.2                         Me       U         CONH.sub.2    T   (CH.sub.2).sub.2                         Me       U         COHCOMe       T   (CH.sub.2).sub.2                         Me       U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         Me       U         Ph            T   (CH.sub.2).sub.2                         Me       U         Bz            T   (CH.sub.2).sub.2                         Me       U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         Me       U         T             T   (CH.sub.2).sub.2                         Et       U         F             T   (CH.sub.2).sub.2                         Et       U         Cl            T   (CH.sub.2).sub.2                         Et       U         Br            T   (CH.sub.2).sub.2                         Et       U         I             T   (CH.sub.2).sub.2                         Et       U         Me            T   (CH.sub.2).sub.2                         Et       U         CF.sub.3      T   (CH.sub.2).sub.2                         Et       U         Et            T   (CH.sub.2).sub.2                         Et       U         n-Pr          T   (CH.sub.2).sub.2                         Et       U         c-Pr          T   (CH.sub.2).sub.2                         Et       U         NO.sub.2      T   (CH.sub.2).sub.2                         Et       U         NH.sub.2      T   (CH.sub.2).sub.2                         Et       U         N(Me)H        T   (CH.sub.2).sub.2                         Et       U         N(Me).sub.2   T   (CH.sub.2).sub.2                         Et       U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         Et       U         N(nPen)H      T   (CH.sub.2).sub.2                         Et       U         NHCOPh        T   (CH.sub.2).sub.2                         Et       U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         Et       U         NHCONHMe      T   (CH.sub.2).sub.2                         Et       U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         Et       U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         Et       U         NHCOBz        T   (CH.sub.2).sub.2                         Et       U         J.sup.1       T   (CH.sub.2).sub.2                         Et       U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         Et       U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         Et       U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         Et       U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         Et       U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         Et       U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         Et       U         N(Me)Ph       T   (CH.sub.2).sub.2                         Et       U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         Et       U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         Et       U         CHO           T   (CH.sub.2).sub.2                         Et       U         CN            T   (CH.sub.2).sub.2                         Et       U         U             T   (CH.sub.2).sub.2                         Et       U         COOMe         T   (CH.sub.2).sub.2                         Et       U         CONH.sub.2    T   (CH.sub.2).sub.2                         Et       U         CONHCOMe      T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         Et       U         Ph            T   (CH.sub.2).sub.2                         Et       U         Bz            T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         Et       U         2-thienyl     T   (CH.sub.2).sub.2                         Et       U         3-furyl       T   (CH.sub.2).sub.2                         Et       U         1-pyrrolyl    T   (CH.sub.2).sub.2                         Et       U         1-imidazolyl  T   (CH.sub.2).sub.2                         Et       U         1-pyrazolyl   T   (CH.sub.2).sub.2                         Et       U         2-pyridyl     T   (CH.sub.2).sub.2                         Et       U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         Et       U         1-piperidyl   T   (CH.sub.2).sub.2                         Et       U         1-piperazinyl T   (CH.sub.2).sub.2                         Et       U         1-morpholinyl T   (CH.sub.2).sub.2                         Et       U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         Et       U         Ph(3-Me)      T   (CH.sub.2)                               Et       U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         Et       U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         Et       U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         Et       U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         Et       U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         Et       U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         Et       U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         Et       U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         Et       U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         Et       U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         Et       U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         Et       U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         Et       U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         Et       U         Ph(3-NHCONH-c-                                                                              T   (CH.sub.2).sub.2                                            Hex)                                                       Et       U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         Et       U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         Et       U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         Et       U         Ph(4-NHCOCF.sup.3)                                                                          T   (CH.sub.2).sub.2                         Et       U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         Et       U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         Et       U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           Et       U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         Et       U         Ph(3-COOH)    T   (CH.sub.2)                               Et       U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         Et       U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         Et       U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         Et       U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         Et       U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         Et       U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         Et       U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         Et       U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         Et       U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         Et       U         OH            T   (CH.sub.2).sub.2                         Et       U         OMe           T   (CH.sub.2).sub.2                         Et       U         OPh           T   (CH.sub.2).sub.2                         Et       U         SH            T   (CH.sub.2).sub.2                         Et       U         SPh           T   (CH.sub.2).sub.2                         Et       U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         Et       U         S-n-Bu        T   (CH.sub.2).sub.2                         Et       U         2-pyrazinyl   T   (CH.sub.2).sub.2                         Et       U         2-pyrimidinyl T   (CH.sub.2).sub.2                         Et       U         3-pyridyl     T   (CH.sub.2).sub.2                         Et       U         4-pyridyl     T   (CH.sub.2).sub.2                         Et       U         T             T   (CH.sub.2).sub.2                         n-Bu     U         F             T   (CH.sub.2).sub.2                         n-Bu     U         Cl            T   (CH.sub.2).sub.2                         n-Bu     U         Br            T   (CH.sub.2).sub.2                         n-Bu     U         I             T   (CH.sub.2).sub.2                         n-Bu     U         Me            T   (CH.sub.2).sub.2                         n-Bu     U         CF.sub.3      T   (CH.sub.2).sub.2                         n-Bu     U         Et            T   (CH.sub.2).sub.2                         n-Bu     U         n-Pr          T   (CH.sub.2).sub.2                         n-Bu     U         c-Pr          T   (CH.sub.2).sub.2                         n-Bu     U         NO.sub.2      T   (CH.sub.2).sub.2                         n-Bu     U         NH.sub.2      T   (CH.sub.2).sub.2                         n-Bu     U         N(Me)H        T   (CH.sub.2).sub.2                         n-Bu     U         N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Bu     U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Bu     U         N(nPen)H      T   (CH.sub.2).sub.2                         n-Bu     U         NHCOPh        T   (CH.sub.2).sub.2                         n-Bu     U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         n-Bu     U         NHCONHMe      T   (CH.sub.2).sub.2                         n-Bu     U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         n-Bu     U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         n-Bu     U         NHCOBz        T   (CH.sub.2).sub.2                         n-Bu     U         J.sup.1       T   (CH.sub.2).sub.2                         n-Bu     U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         n-Bu     U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         n-Bu     U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         n-Bu     U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         n-Bu     U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         n-Bu     U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         n-Bu     U         N(Me)Ph       T   (CH.sub.2).sub.2                         n-Bu     U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.3).sub.2                         n-Bu     U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Bu     U         CHO           T   (CH.sub.2).sub.2                         n-Bu     U         CN            T   (CH.sub.2).sub.2                         n-Bu     U         U             T   (CH.sub.2).sub.2                         n-Bu     U         COOMe         T   (CH.sub.2).sub.2                         n-Bu     U         CONH.sub.2    T   (CH.sub.2).sub.2                         n-Bu     U         CONHCOMe      T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Bu     U         Ph            T   (CH.sub.2).sub.2                         n-Bu     U         Bz            T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Bu     U         2-thienyl     T   (CH.sub.2).sub.2                         n-Bu     U         3-furyl       T   (CH.sub.2).sub.2                         n-Bu     U         1-pyrrolyl    T   (CH.sub.2).sub.2                         n-Bu     U         1-imidazolyl  T   (CH.sub.2).sub.2                         n-Bu     U         1-pyrazolyl   T   (CH.sub.2).sub.2                         n-Bu     U         2-pyridyl     T   (CH.sub.2).sub.2                         n-Bu     U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         n-Bu     U         1-piperidyl   T   (CH.sub.2).sub.2                         n-Bu     U         1-piperazinyl T   (CH.sub.2).sub.2                         n-Bu     U         4-morpholinyl T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-Me)      T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-N-(nPen)COPh)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           n-Bu     U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         n-Bu     U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-CH.sub.2 OH)                                          n-Bu     U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         n-Bu     U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         n-Bu     U         Ph(4-CH.sub..sub.2 COOH)                                                                    T   (CH.sub.2).sub.2                         n-Bu     U         Ph (4-Ph)     T   (CH.sub.2).sub.2                         n-Bu     U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         n-Bu     U         OH            T   (CH.sub.2).sub.2                         n-Bu     U         OMe           T   (CH.sub.2).sub.2                         n-Bu     U         OPh           T   (CH.sub.2).sub.2                         n-Bu     U         SH            T   (CH.sub.2).sub.2                         n-Bu     U         SPh           T   (CH.sub.2).sub.2                         n-Bu     U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         n-Bu     U         S-n-Bu        T   (CH.sub.2).sub.2                         n-Bu     U         2-pyrazinyl   T   (CH.sub.2).sub.2                         n-Bu     U         2-pyrimidinyl T   (CH.sub.2).sub.2                         n-Bu     U         3-pyridyl     T   (CH.sub.2).sub.2                         n-Bu     U         4-pyridyl     T   (CH.sub.2).sub.2                         n-Bu     U         T             T   (CH.sub.2).sub.2                         c-Pr     U         F             T   (CH.sub.2).sub.2                         c-Pr     U         Cl            T   (CH.sub.2).sub.2                         c-Pr     U         Br            T   (CH.sub.2).sub.2                         c-Pr     U         I             T   (CH.sub.2).sub.2                         c-Pr     U         Me            T   (CH.sub.2).sub.2                         c-Pr     U         CF.sub.3      T   (CH.sub.2).sub.2                         c-Pr     U         Et            T   (CH.sub.2).sub.2                         c-Pr     U         n-Pr          T   (CH.sub.2).sub.2                         c-Pr     U         c-Pr          T   (CH.sub.2).sub.2                         c-Pr     U         NO.sub.2      T   (CH.sub.2).sub.2                         c-Pr     U         NH.sub.2      T   (CH.sub.2).sub.2                         c-Pr     U         N(Me)H        T   (CH.sub.2).sub.2                         c-Pr     U         N(Me).sub.2   T   (CH.sub.2).sub.2                         c-Pr     U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         c-Pr     U         N(nPen)H      T   (CH.sub.2).sub.2                         c-Pr     U         NHCOPh        T   (CH.sub.2).sub.2                         c-Pr     U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         c-Pr     U         NHCONHMe      T   (CH.sub.2).sub.2                         c-Pr     U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         c-Pr     U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         c-Pr     U         NHCOBz        T   (CH.sub.2).sub.2                         c-Pr     U         J.sup.1       T   (CH.sub.3).sub.2                         c-Pr     U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         c-Pr     U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         c-Pr     U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         c-Pr     U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         c-Pr     U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         c-Pr     U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         c-Pr     U         N(Me)Ph       T   (CH.sub.2).sub.2                         c-Pr     U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         c-Pr     U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         c-Pr     U         CHO           T   (CH.sub.2).sub.2                         c-Pr     U         U             T   (CH.sub.2).sub.2                         c-Pr     U         COOMe         T   (CH.sub.2).sub.2                         c-Pr     U         CONH.sub.2    T   (CH.sub.2).sub.2                         c-Pr     U         CONHCOMe      T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 CONHPh                                            c-Pr     U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         c-Pr     U         Ph            T   (CH.sub.2).sub.2                         c-Pr     U         Bz            T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         c-Pr     U         2-thienyl     T   (CH.sub.2).sub.2                         c-Pr     U         3-furyl       T   (CH.sub.2).sub.2                         c-Pr     U         1-pyrrolyl    T   (CH.sub.2).sub.2                         c-Pr     U         1-imidazolyl  T   (CH.sub.2).sub.2                         c-Pr     U         1-pyrazolyl   T   (CH.sub.2).sub.2                         c-Pr     U         2-pyridyl     T   (CH.sub.2).sub.2                         c-Pr     U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         c-Pr     U         1-piperidyl   T   (CH.sub.2).sub.2                         c-Pr     U         1-piperazinyl T   (CH.sub.2).sub.2                         c-Pr     U         4-morpholinyl T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-Me)      T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         c-Pr     U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           c-Pr     U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         c-Pr     U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         c-Pr     U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         c-Pr     U         PH(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         c-Pr     U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         c-Pr     U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         c-Pr     U         OH            T   (CH.sub.2).sub.2                         c-Pr     U         OMe           T   (CH.sub.2).sub.2                         c-Pr     U         OPh           T   (CH.sub.2).sub.2                         c-Pr     U         SH            T   (CH.sub.2).sub.2                         c-Pr     U         SPh           T   (CH.sub.2).sub.2                         c-Pr     U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         c-Pr     U         S-n-Bu        T   (CH.sub.2).sub.2                         c-Pr     U         2-pyrazinyl   T   (CH.sub.2).sub.2                         c-Pr     U         2-pyrimidinyl T   (CH.sub.2).sub.2                         c-Pr     U         3-pyridyl     T   (CH.sub.2).sub.2                         c-Pr     U         4-pyridyl     T   (CH.sub.2).sub.2                         c-Pr     U         T             T   (CH.sub.2).sub.2                         i-Pr     U         F             T   (CH.sub.2).sub.2                         i-Pr     U         Cl            T   (CH.sub.2).sub.2                         i-Pr     U         Br            T   (CH.sub.2).sub.2                         i-Pr     U         I             T   (CH.sub.2).sub.2                         i-Pr     U         Me            T   (CH.sub.2).sub.2                         i-Pr     U         CF.sub.3      T   (CH.sub.2).sub.2                         i-Pr     U         Et            T   (CH.sub.2).sub.2                         i-Pr     U         n-Pr          T   (CH.sub.2).sub.2                         i-Pr     U         c-Pr          T   (CH.sub.2).sub.2                         i-Pr     U         NO.sub.2      T   (CH.sub.2).sub.2                         i-Pr     U         NH.sub.2      T   (CH.sub.2).sub.2                         i-Pr     U         N(Me)H        T   (CH.sub.2).sub.2                         i-Pr     U         N(Me).sub.2   T   (CH.sub.2).sub.2                         i-Pr     U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         i-Pr     U         N(nPen)H      T   (CH.sub.2).sub.2                         i-Pr     U         NHCOPh        T   (CH.sub.2).sub.2                         i-Pr     U         J.sup.1       T   (CH.sub.2).sub.2                         i-Pr     U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         i-Pr     U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         i-Pr     U         CHO           T   (CH.sub.2).sub.2                         i-Pr     U         CN            T   (CH.sub.2).sub.2                         i-Pr     U         U             T   (CH.sub.2).sub.2                         i-Pr     U         COOMe         T   (CH.sub.2).sub.2                         i-Pr     U         CONH.sub.2    T   (CH.sub.2).sub.2                         i-Pr     U         CONHCOMe      T   (CH.sub.2).sub.2                         i-Pr     U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         i-Pr     U         Ph            T   (CH.sub.2).sub.2                         i-Pr     U         Bz            T   (CH.sub.2).sub.2                         i-Pr     U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     T         F             T   (CH.sub.2).sub.2                         n-Pr     T         Cl            T   (CH.sub.2).sub.2                         n-Pr     T         Br            T   (CH.sub.2).sub.2                         n-Pr     T         I             T   (CH.sub.2).sub.2                         n-Pr     T         Me            T   (CH.sub.2).sub.2                         n-Pr     T         CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     T         Et            T   (CH.sub.2).sub.2                         n-Pr     T         n-Pr          T   (CH.sub.2).sub.2                         n-Pr     T         c-Pr          T   (CH.sub.2).sub.2                         n-Pr     T         NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     T         NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     T         N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     T         N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     T         N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     T         N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     T         NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     T         J.sup.1       T   (CH.sub.2).sub.2                         n-Pr     T         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     T         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     T         CHO           T   (CH.sub.2).sub.2                         n-Pr     T         CN            T   (CH.sub.2).sub.2                         n-Pr     T         U             T   (CH.sub.2).sub.2                         n-Pr     T         COOMe         T   (CH.sub.2).sub.2                         n-Pr     T         CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     T         CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     T         CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     T         Ph            T   (CH.sub.2).sub.2                         n-Pr     T         Bz            T   (CH.sub.2).sub.2                         n-Pr     T         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     T         T             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         F             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Cl            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Br            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         I             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Me            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CF.sub.3      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Et            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Br            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         I             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Me            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CF.sub.3      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Et            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         n-Pr          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         c-Pr          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NO.sub.2      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NH.sub.2      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me)H        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me).sub.2   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(nPen)H      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCOPh        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCONHMe      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCOBz        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         J.sup.1       T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         N(Me)Ph       T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CHO           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CN            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         U             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         COOMe         T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CONH.sub.2    T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CONHCOMe      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Bz            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         2-thienyl     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         3-furyl       T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-pyrrolyl    T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-imidazolyl  T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-pyrazolyl   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         2-pyridyl     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-piperidyl   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         1-piperazinyl T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         4-morpholinyl T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-Me)      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              1-Propenyl                                                                             U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-NHC(NH)NH.sub.2)                                                                       T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         1-Propenyl                                                                             U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         OH            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         OMe           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         OPh           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         SH            T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         SPh           T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         S-n-Bu        T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         2-pyrazinyl   T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         2-pyrimidinyl T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         3-pyridyl     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         4-pyridyl     T   (CH.sub.2).sub.2                         1-Propenyl                                                                             U         T             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         F             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Cl            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Br            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         I             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Me            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CF.sub.3      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Et            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         n-Pr          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         c-Pr          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NO.sub.2      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NH.sub.2      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(ME)H        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(Me).sub.2   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(nPen)H      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCOPh        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCONHMe      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCOBz        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         J.sup.1       T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         N(Me)Ph       T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CHO           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CN            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         U             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         COOMe         T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CONH.sub.2    T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CONHCOMe      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Bz            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         2-thienyl     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         3-furyl       T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-pyrrolyl    T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-imidazolyl  T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-pyrazolyl   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         2-pyridyl     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-piperidyl   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         1-piperazinyl T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         4-morpholinyl T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-Me)      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              2-Propenyl                                                                             U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           2-Propenyl                                                                             U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         2-Propenyl                                                                             U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         OH            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         OMe           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         OPh           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         SH            T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         SPh           T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         S-n-Bu        T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         2-pyrazinyl   T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         2-pyrimidinyl T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         3-pyridyl     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         4-pyridyl     T   (CH.sub.2).sub.2                         2-Propenyl                                                                             U         T             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         F             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Cl            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Br            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         I             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Me            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CF.sub.3      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Et            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         n-Pr          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         c-Pr          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         NO.sub.2      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         NH.sub.2      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         N(Me)H        T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         N(Me).sub.2   T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         N(nPen)H      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         NHCOPh        T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         J.sup.1       T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CHO           T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CN            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         U             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         COOMe         T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CONH.sub.2    T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CONHCOMe      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Bz            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         2-thienyl     T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         3-furyl       T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph-4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              1-Butenyl                                                                              U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           1-Butenyl                                                                              U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         1-Butenyl                                                                              U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         OH            T   (CH.sub.2).sub.2                         1-Butenyl                                                                              U         T             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         F             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Cl            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Br            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         I             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Me            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CF.sub.3      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Et            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         n-Pr          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         c-Pr          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         NO.sub.2      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         NH.sub.2      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(Me)H        T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(Me).sub.2   T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(nPen)H      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         NHCOPh        T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         NHCONHMe      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         J.sup.1       T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CHO           T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CN            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         U             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         COOMe         T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CONH.sub.2    T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CONHCOMe      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Bz            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         2-thienyl     T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         3-furyl       T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              2-Butenyl                                                                              U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-NHCOCF.sub.2)                                                                          T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           2-Butenyl                                                                              U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         2-Butenyl                                                                              U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         2-Butenyl                                                                              U         T             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         F             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Cl            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Br            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         I             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Me            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CF.sub.3      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Et            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         n-Pr          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         c-Pr          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         NO.sub.2      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         NH.sub.2      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         N(Me)H        T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         N(Me).sub.2   T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         N(nPen)H      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         NHCOPh        T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         J.sup.1       T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CHO           T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CN            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         U             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         COOMe         T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CONH.sub.2    T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CONHCOMe      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Bz            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         2-thienyl     T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         3-furyl       T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHCONH-c-Hex)                                              3-Butenyl                                                                              U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           3-Butenyl                                                                              U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         3-Butenyl                                                                              U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         3-Butenyl                                                                              U         T             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         F             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Cl            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Br            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         I             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Me            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CF.sub.3      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Et            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         n-Pr          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         c-Pr          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NO.sub.2      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NH.sub.2      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me)H        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me).sub.2   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me)n-Bu     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(nPen)H      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCOPh        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me)CO-c-Hex T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCONHMe      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me)CONHPh   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCONH-c-Hex  T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCOBz        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         J.sup.1       T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NBzCO-n-Bu    T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NBzCOO-i-Bu   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCO-n-Bu     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCOO-i-Bu    T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHCOCF.sub.3  T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHSO.sub.2 CF.sub.3                                                                         T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         N(Me)Ph       T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CHO           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CN            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         U             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         COOMe         T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CONH.sub.2    T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CONHCOMe      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 OH   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 COOH T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Bz            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         2-thienyl     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         3-furyl       T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-pyrrolyl    T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-imidazolyl  T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-pyrazolyl   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-pyridyl     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-pyrrolidinyl                                                                              T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-piperazinyl T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         1-morpholinyl T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl)      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-Me)      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-OMe)     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-NO.sub.2)                                                                              T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NH.sub.2)                                                                              T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NMe.sub.2)                                                                             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-J.sup.2) T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl,3-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl,4-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl,5-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(2-Cl,6-J.sup.1)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NHCOPh)  T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NHCO-c-Hex)                                                                            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NHCONHMe)                                                                              T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NMeCONHPh)                                                                             T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NHCONH-c-Hex)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NHCOBz)  T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-N(nPen)COPh)                                                                           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NHCOnBu) T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NHCOCF.sub.3)                                                                          T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-NHSO.sub.2 CF.sub.3)                                                                   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-NMePh)   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-         T   (CH.sub.2).sub.2                                            NHC(NH)NH.sub.2)                                           C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-C(NH)NH.sub.2)                                                                         T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-COOH)    T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-CONH.sub.2)                                                                            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(3-CH.sub.2 NH.sub.2)                                                                     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-CH.sub.2 OH)                                                                           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-CH.sub.2 J.sup.2)                                                                      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-         T   (CH.sub.2).sub.2                                            CH.sub.2 NHCONHMe)                                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-CH.sub.2 CONHPh)                                                                       T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-CH.sub.2 COOH)                                                                         T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         Ph(4-Ph)      T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         CH.sub.2 CH.sub.2 Ph(2-Cl,5-J.sup.1)                                                        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         OH            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         OMe           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         OPh           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         SH            T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         SPh           T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         SO.sub.2 Ph   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         S-n-Bu        T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         2-pyrazinyl   T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         2-pyrimidinyl T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         3-pyridyl     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         4-pyridyl     T   (CH.sub.2).sub.2                         C.sub.2 H.sub.5 CH(OH)                                                                 U         T             T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             F             T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Cl            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Br            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             I             T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Me            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Et            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             n-Pr          T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             c-Pr          T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CHO           T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CN            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             U             T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             COOMe         T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Ph            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             Bz            T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             2-thienyl     T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             3-furyl       T   (CH.sub.2).sub.2                         n-Pr     CH.sub.2 OH                                                                             T             T   (CH.sub.2).sub.2                         n-Pr     CHO       F             T   (CH.sub.2).sub.2                         n-Pr     CHO       Cl            T   (CH.sub.2).sub.2                         n-Pr     CHO       Br            T   (CH.sub.2).sub.2                         n-Pr     CHO       I             T   (CH.sub.2).sub.2                         n-Pr     CHO       Me            T   (CH.sub.2).sub.2                         n-Pr     CHO       CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     CHO       Et            T   (CH.sub.2).sub.2                         n-Pr     CHO       n-Pr          T   (CH.sub.2).sub.2                         n-Pr     CHO       c-Pr          T   (CH.sub.2).sub.2                         n-Pr     CHO       NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     CHO       NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     CHO       N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     CHO       N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     CHO       N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     CHO       N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     CHO       NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     CHO       NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     CHO       C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     CHO       CHO           T   (CH.sub.2).sub.2                         n-Pr     CHO       CN            T   (CH.sub.2).sub.2                         n-Pr     CHO       U             T   (CH.sub.2).sub.2                         n-Pr     CHO       COOMe         T   (CH.sub.2).sub.2                         n-Pr     CHO       CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     CHO       CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 NH.sub.2                                                                           T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 OH   T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 NHCOPh                                                                             T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 N(nPen)COPh                                                                        T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 NHCONHMe                                                                           T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 CONHPh                                                                             T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     CHO       Ph            T   (CH.sub.2).sub.2                         n-Pr     CHO       Bz            T   (CH.sub.2).sub.2                         n-Pr     CHO       CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     CHO       2-thienyl     T   (CH.sub.2).sub.2                         n-Pr     CHO       3-furyl       T   (CH.sub.2).sub.2                         n-Pr     CHO       T             T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            F             T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Cl            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Br            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            I             T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Me            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Et            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            n-Pr          T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            c-Pr          T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CHO           T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CN            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            U             T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            COOMe         T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Ph            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            Bz            T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            2-thienyl     T   (CH.sub.2).sub.2                         n-Pr     NHCOCF.sub.3                                                                            3-furyl       T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  T             T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  F             T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Cl            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Br            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  I             T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Me            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CF.sub.3      T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Et            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  n-Pr          T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  c-Pr          T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  NO.sub.2      T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  NH.sub.2      T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  N(Me)H        T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  N(Me).sub.2   T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  N(Me)n-Bu     T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  N(nPen)H      T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  NHCOPh        T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  NHC(NH)NH.sub.2                                                                             T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  C(NH)NH.sub.2 T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CHO           T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CN            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  U             T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  COOMe         T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CONH.sub.2    T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CONHCOMe      T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CH.sub.2 COOH T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Ph            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  Bz            T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  CH.sub.2 CH.sub.2 Ph                                                                        T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  2-thienyl     T   (CH.sub.2).sub.2                         n-Pr     NH.sub.2  3-furyl       T   (CH.sub.2).sub.2                         ______________________________________                                    

                  TABLE 2                                                         ______________________________________                                         ##STR27##                                                                    R.sup.3    R.sup.4 R.sup.5                                                                              R.sup.6                                                                             R.sup.7                                                                            Y     Z                                  ______________________________________                                        F          Me      H      H     T    CH    CH                                 Cl         Me      H      H     T    CH    CH                                 Br         Me      H      H     T    CH    CH                                 I          Me      H      H     T    CH    CH                                 Me         Me      H      H     T    CH    CH                                 CF.sub.3   Me      H      H     T    CH    CH                                 Et         Me      H      H     T    CH    CH                                 n-Pr       Me      H      H     T    CH    CH                                 c-Pr       Me      H      H     T    CH    CH                                 NO.sub.2   Me      H      H     T    CH    CH                                 NH.sub.2   Me      H      H     T    CH    CH                                 N(Me)H     Me      H      H     T    CH    CH                                 N(Me).sub.2                                                                              Me      H      H     T    CH    CH                                 N(Me)n-Bu  Me      H      H     T    CH    CH                                 N(nPen)H   Me      H      H     T    CH    CH                                 NHCOPh     Me      H      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          Me      H      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            Me      H      H     T    CH    CH                                 CHO        Me      H      H     T    CH    CH                                 CN         Me      H      H     T    CH    CH                                 U          Me      H      H     T    CH    CH                                 COOMe      Me      H      H     T    CH    CH                                 CONH.sub.2 Me      H      H     T    CH    CH                                 CONHCOMe   Me      H      H     T    CH    CH                                 Ph         Me      H      H     T    CH    CH                                 Bz         Me      H      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     Me      H      H     T    CH    CH                                 2-thienyl  Me      H      H     T    CH    CH                                 3-furyl    Me      H      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            Me      H      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      Me      H      H     T    CH    CH                                 T          Me      H      H     T    CH    CH                                 F          F       H      H     T    CH    CH                                 Cl         F       H      H     T    CH    CH                                 Br         F       H      H     T    CH    CH                                 I          F       H      H     T    CH    CH                                 Me         F       H      H     T    CH    CH                                 CF.sub.3   F       H      H     T    CH    CH                                 Et         F       H      H     T    CH    CH                                 n-Pr       F       H      H     T    CH    CH                                 c-Pr       F       H      H     T    CH    CH                                 NO.sub.2   F       H      H     T    CH    CH                                 NH.sub.2   F       H      H     T    CH    CR                                 N(Me)H     F       H      H     T    CH    CH                                 N(Me).sub.2                                                                              F       H      H     T    CH    CH                                 N(Me)n-Bu  F       H      H     T    CH    CH                                 N(nPen)H   F       H      H     T    CH    CH                                 NHCOPh     F       H      H     T    CH    CH                                 J.sup.1    F       H      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          F       H      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            F       H      H     T    CH    CH                                 CHO        F       H      H     T    CH    CH                                 CN         F       H      H     T    CH    CH                                 U          F       H      H     T    CH    CH                                 COOMe      F       H      H     T    CH    CH                                 CONH.sub.2 F       H      H     T    CH    CH                                 CONHCOMe   F       H      H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     F       H      H     T    CH    CH                                 Ph         F       H      H     T    CH    CH                                 Bz         F       H      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     F       H      H     T    CH    CH                                 2-thienyl  F       H      H     T    CH    CH                                 3-furyl    F       H      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            F       H      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      F       H      H     T    CH    CH                                 T          F       H      H     T    CH    CH                                 F          Cl      H      H     T    CH    CH                                 Cl         Cl      H      H     T    CH    CH                                 Br         Cl      H      H     T    CH    CH                                 I          Cl      H      H     T    CH    CH                                 Me         Cl      H      H     T    CH    CH                                 CF.sub.3   Cl      H      H     T    CH    CH                                 Et         Cl      H      H     T    CH    CH                                 n-Pr       Cl      H      H     T    CH    CH                                 c-Pr       Cl      H      H     T    CH    CH                                 NO.sub.2   Cl      H      H     T    CH    CH                                 NH.sub.2   Cl      H      H     T    CH    CH                                 N(Me)H     Cl      H      H     T    CH    CH                                 N(Me).sub.2                                                                              Cl      H      H     T    CH    CH                                 N(Me)n-Bu  Cl      H      H     T    CH    CH                                 N(nPen)H   Cl      H      H     T    CH    CH                                 NHCOPh     Cl      H      H     T    CH    CH                                 J.sup.1    Cl      H      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          Cl      H      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            Cl      H      H     T    CH    CH                                 CHO        Cl      H      H     T    CH    CH                                 CN         Cl      H      H     T    CH    CH                                 U          Cl      H      H     T    CH    CH                                 COOMe      Cl      H      H     T    CH    CH                                 CONH.sub.2 Cl      H      H     T    CH    CH                                 CONHCOMe   Cl      H      H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     Cl      H      H     T    CH    CH                                 Ph         Cl      H      H     T    CH    CH                                 Bz         Cl      H      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     Cl      H      H     T    CH    CH                                 2-thienyl  Cl      H      H     T    CH    CH                                 3-furyl    Cl      H      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            Cl      H      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      Cl      H      H     T    CH    CH                                 T          Cl      H      H     T    CH    CH                                 F          Br      H      H     T    CH    CH                                 Cl         Br      H      H     T    CH    CH                                 Br         Br      H      H     T    CH    CH                                 I          Br      H      H     T    CH    CH                                 Me         Br      H      H     T    CH    CH                                 CF.sub.3   Br      H      H     T    CH    CH                                 Et         Br      H      H     T    CH    CH                                 n-Pr       Br      H      H     T    CH    CH                                 c-Pr       Br      H      H     T    CH    CH                                 NO.sub.2   Br      H      H     T    CH    CH                                 NH.sub.2   Br      H      H     T    CH    CH                                 N(Me)H     Br      H      H     T    CH    CH                                 N(Me).sub.2                                                                              Br      H      H     T    CH    CH                                 N(Me)n-Bu  Br      H      H     T    CH    CH                                 N(nPen)H   Br      H      H     T    CH    CH                                 NHCOPh     Br      H      H     T    CH    CH                                 J.sup.1    Br      H      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          Br      H      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            Br      H      H     T    CH    CH                                 CHO        Br      H      H     T    CH    CH                                 CN         Br      H      H     T    CH    CH                                 U          Br      H      H     T    CH    CH                                 COOMe      Br      H      H     T    CH    CH                                 CONH.sub.2 Br      H      H     T    CH    CH                                 CONHCOMe   Br      H      H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     Br      H      H     T    CH    CH                                 Ph         Br      H      H     T    CH    CH                                 Bz         Br      H      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     Br      H      H     T    CH    CH                                 2-thienyl  Br      H      H     T    CH    CH                                 3-furyl    Br      H      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            Br      H      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      Br      H      H     T    CH    CH                                 T          Br      H      H     T    CH    CH                                 F          OH      H      H     T    CH    CH                                 Cl         OH      H      H     T    CH    CH                                 Br         OH      H      H     T    CH    CH                                 I          OH      H      H     T    CH    CH                                 Me         OH      H      H     T    CH    CH                                 CF.sub.3   OH      H      H     T    CH    CH                                 Et         OH      H      H     T    CH    CH                                 n-Pr       OH      H      H     T    CH    CH                                 c-Pr       OH      H      H     T    CH    CH                                 NO.sub.2   OH      H      H     T    CH    CH                                 NH.sub.2   OH      H      H     T    CH    CH                                 N(Me)H     OH      H      H     T    CH    CH                                 N(Me).sub.2                                                                              OH      H      H     T    CH    CH                                 N(Me)n-Bu  OH      H      H     T    CH    CH                                 N(nPen)H   OH      H      H     T    CH    CH                                 NHCOPh     OH      H      H     T    CH    CH                                 J.sup.1    OH      H      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          OH      H      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            OH      H      H     T    CH    CH                                 CHO        OH      H      H     T    CH    CH                                 CN         OH      H      H     T    CH    CH                                 U          OH      H      H     T    CH    CH                                 COOMe      OH      H      H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     OH      H      H     T    CH    CH                                 Ph         OH      H      H     T    CH    CH                                 Bz         OH      H      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     OH      H      H     T    CH    CH                                 2-thienyl  OH      H      H     T    CH    CH                                 3-furyl    OH      H      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            OH      H      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      OH      H      H     T    CH    CH                                 T          OH      H      H     T    CH    CH                                 F          H       H      H     T    CMe   CH                                 Cl         H       H      H     T    CMe   CH                                 Br         H       H      H     T    CMe   CH                                 I          H       H      H     T    CMe   CH                                 Me         H       H      H     T    CMe   CH                                 CF.sub.3   H       H      H     T    CMe   CH                                 Et         H       H      H     T    CMe   CH                                 n-Pr       H       H      H     T    CMe   CH                                 c-Pr       H       H      H     T    CMe   CH                                 NO.sub.2   H       H      H     T    CMe   CH                                 NH.sub.2   H       H      H     T    CMe   CH                                 N(Me)H     H       H      H     T    CMe   CH                                 N(Me).sub.2                                                                              H       H      H     T    CMe   CH                                 N(Me)n-Bu  H       H      H     T    CMe   CH                                 N(nPen)H   H       H      H     T    CMe   CH                                 NHCOPh     H       H      H     T    CMe   CH                                 J.sup.1    H       H      H     T    CMe   CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    CMe   CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    CMe   CH                                 CHO        H       H      H     T    CMe   CH                                 CN         H       H      H     T    CMe   CH                                 U          H       H      H     T    CMe   CH                                 COOMe      H       H      H     T    CMe   CH                                 CONH.sub.2 H       H      H     T    CMe   CH                                 CONHCOMe   H       H      H     T    CMe   CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CMe   CH                                 Ph         H       H      H     T    CMe   CH                                 Bz         H       H      H     T    CMe   CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CMe   CH                                 2-thienyl  H       H      H     T    CMe   CH                                 3-furyl    H       H      H     T    CMe   CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    CMe   CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CMe   CH                                 T          H       H      H     T    CMe   CH                                 F          H       H      H     T    CF    CH                                 Cl         H       H      H     T    CF    CH                                 Br         H       H      H     T    CF    CH                                 I          H       H      H     T    CF    CH                                 Me         H       H      H     T    CF    CH                                 CF.sub.3   H       H      H     T    CF    CH                                 Et         H       H      H     T    CF    CH                                 n-Pr       H       H      H     T    CF    CH                                 c-Pr       H       H      H     T    CF    CH                                 NO.sub.2   H       H      H     T    CF    CH                                 NH.sub.2   H       H      H     T    CF    CH                                 N(Me)H     H       H      H     T    CF    CH                                 N(Me).sub.2                                                                              H       H      H     T    CF    CH                                 N(Me)n-Bu  H       H      H     T    CF    CH                                 N(nPen)H   H       H      H     T    CF    CH                                 NHCOPh     H       H      H     T    CF    CH                                 J.sup.1    H       H      H     T    CF    CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    CF    CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    CF    CH                                 CHO        H       H      H     T    CF    CH                                 CN         H       H      H     T    CF    CH                                 U          H       H      H     T    CF    CH                                 COOMe      H       H      H     T    CF    CH                                 CONH.sub.2 H       H      H     T    CF    CH                                 CONHCOMe   H       H      H     T    CF    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CF    CH                                 Ph         H       H      H     T    CF    CH                                 Bz         H       H      H     T    CF    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CF    CH                                 2-thienyl  H       H      H     T    CF    CH                                 3-furyl    H       H      H     T    CF    CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    CF    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CF    CH                                 T          H       H      H     T    CF    CH                                 F          H       H      H     T    CCl   CH                                 Cl         H       H      H     T    CCl   CH                                 Br         H       H      H     T    CCl   CH                                 I          H       H      H     T    CCl   CH                                 Me         H       H      H     T    CCl   CH                                 CF.sub.3   H       H      H     T    CCl   CH                                 Et         H       H      H     T    CCl   CH                                 n-Pr       H       H      H     T    CCl   CH                                 c-Pr       H       H      H     T    CCl   CH                                 NO.sub.2   H       H      H     T    CCl   CH                                 NH.sub.2   H       H      H     T    CCl   CH                                 N(Me)H     H       H      H     T    CCl   CH                                 N(Me).sub.2                                                                              H       H      H     T    CCl   CH                                 N(Me)n-Bu  H       H      H     T    CCl   CH                                 N(nPen)H   H       H      H     T    CCl   CH                                 NHCOPh     H       H      H     T    CCl   CH                                 J.sup.1    H       H      H     T    CCl   CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    CCl   CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    CCl   CH                                 CHO        H       H      H     T    CCl   CH                                 CN         H       H      H     T    CCl   CH                                 U          H       H      H     T    CCl   CH                                 COOMe      H       H      H     T    CCl   CH                                 CONH.sub.2 H       H      H     T    CCl   CH                                 CONHCOMe   H       H      H     T    CCl   CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CCl   CH                                 Ph         H       H      H     T    CCl   CH                                 Bz         H       H      H     T    CCl   CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CCl   CH                                 2-thienyl  H       H      H     T    CCl   CH                                 3-furyl    H       H      H     T    CCl   CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    CCl   CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CCl   CH                                 T          H       H      H     T    CCl   CH                                 F          H       H      H     T    CBr   CH                                 Cl         H       H      H     T    CBr   CH                                 Br         H       H      H     T    CBr   CH                                 I          H       H      H     T    CBr   CH                                 Me         H       H      H     T    CBr   CH                                 CF.sub.3   H       H      H     T    CBr   CH                                 Et         H       H      H     T    CBr   CH                                 n-Pr       H       H      H     T    CBr   CH                                 c-Pr       H       H      H     T    CBr   CH                                 NO.sub.2   H       H      H     T    CBr   CH                                 NH.sub.2   H       H      H     T    CBr   CH                                 N(Me)H     H       H      H     T    CBr   CH                                 N(Me).sub.2                                                                              H       H      H     T    CBr   CH                                 N(Me)n-Bu  H       H      H     T    CBr   CH                                 N(nPen)H   H       H      H     T    CBr   CH                                 NHCOPh     H       H      H     T    CBr   CH                                 J.sup.1    H       H      H     T    CBr   CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    CBr   CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    CBr   CH                                 CHO        H       H      H     T    CBr   CH                                 CN         H       H      H     T    CBr   CH                                 U          H       H      H     T    CBr   CH                                 COOMe      H       H      H     T    CBr   CH                                 CONH.sub.2 H       H      H     T    CBr   CH                                 CONHCOMe   H       H      H     T    CBr   CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CBr   CH                                 Ph         H       H      H     T    CBr   CH                                 Bz         H       H      H     T    CBr   CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CBr   CH                                 2-thienyl  H       H      H     T    CBr   CH                                 3-furyl    H       H      H     T    CBr   CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    CBr   CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CBr   CH                                 T          H       H      H     T    CBr   CH                                 F          H       H      H     T    COH   CH                                 Cl         H       H      H     T    COH   CH                                 Br         H       H      H     T    COH   CH                                 I          H       H      H     T    COH   CH                                 Me         H       H      H     T    COH   CH                                 CF.sub.3   H       H      H     T    COH   CH                                 Et         H       H      H     T    COH   CH                                 n-Pr       H       H      H     T    COH   CH                                 c-Pr       H       H      H     T    COH   CH                                 NO.sub.2   H       H      H     T    COH   CH                                 NH.sub.2   H       H      H     T    COH   CH                                 N(Me)H     H       H      H     T    COH   CH                                 N(Me).sub.2                                                                              H       H      H     T    COH   CH                                 N(Me)n-Bu  H       H      H     T    COH   CH                                 N(nPen)H   H       H      H     T    COH   CH                                 NHCOPh     H       H      H     T    COH   CH                                 J.sup.1    H       H      H     T    COH   CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    COH   CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    COH   CH                                 CHO        H       H      H     T    COH   CH                                 CN         H       H      H     T    COH   CH                                 U          H       H      H     T    COH   CH                                 COOMe      H       H      H     T    COH   CH                                 CONH.sub.2 H       H      H     T    COH   CH                                 CONHCOMe   H       H      H     T    COH   CH                                 Ph         H       H      H     T    COH   CH                                 Bz         H       H      H     T    COH   CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    COH   CH                                 2-thienyl  H       H      H     T    COH   CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    COH   CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    COH   CH                                 T          H       H      H     T    COH   CH                                 F          H       H      H     T    N     CH                                 Cl         H       H      H     T    N     CH                                 Br         H       H      H     T    N     CH                                 I          H       H      H     T    N     CH                                 Me         H       H      H     T    N     CH                                 CF.sub.3   H       H      H     T    N     CH                                 Et         H       H      H     T    N     CH                                 n-Pr       H       H      H     T    N     CH                                 c-Pr       H       H      H     T    N     CH                                 NO.sub.2   H       H      H     T    N     CH                                 NH.sub.2   H       H      H     T    N     CH                                 N(Me)H     H       H      H     T    N     CH                                 N(Me).sub.2                                                                              H       H      H     T    N     CH                                 N(Me)n-Bu  H       H      H     T    N     CH                                 N(nPen)H   H       H      H     T    N     CH                                 NHCOPh     H       H      H     T    N     CH                                 J.sup.1    H       H      H     T    N     CH                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    N     CH                                 C(NH)NH.sub.2                                                                            H       H      H     T    N     CH                                 CHO        H       H      H     T    N     CH                                 CN         H       H      H     T    N     CH                                 U          H       H      H     T    N     CH                                 COOMe      H       H      H     T    N     CH                                 CONH.sub.2 H       H      H     T    N     CH                                 CONHCOMe   H       H      H     T    N     CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    N     CH                                 Ph         H       H      H     T    N     CH                                 Bz         H       H      H     T    N     CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    N     CH                                 2-thienyl  H       H      H     T    N     CH                                 3-furyl    H       H      H     T    N     CH                                 Ph(4-J.sup.2)                                                                            H       H      H     T    N     CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    N     CH                                 T          H       H      H     T    N     CH                                 F          H       Me     H     T    CH    CH                                 Cl         H       Me     H     T    CH    CH                                 Br         H       Me     H     T    CH    CH                                 I          H       Me     H     T    CH    CH                                 Me         H       Me     H     T    CH    CH                                 CF.sub.3   H       Me     H     T    CH    CH                                 Et         H       Me     H     T    CH    CH                                 n-Pr       H       Me     H     T    CH    CH                                 c-Pr       H       Me     H     T    CH    CH                                 NO.sub.2   H       Me     H     T    CH    CH                                 NH.sub.2   H       Me     H     T    CH    CH                                 N(Me)H     H       Me     H     T    CH    CH                                 N(Me).sub.2                                                                              H       Me     H     T    CH    CH                                 N(Me)n-Bu  H       Me     H     T    CH    CH                                 N(nPen)H   H       Me     H     T    CH    CH                                 NHCOPh     H       Me     H     T    CH    CH                                 J.sup.1    H       Me     H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       Me     H     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       Me     H     T    CH    CH                                 CHO        H       Me     H     T    CH    CH                                 CN         H       Me     H     T    CH    CH                                 U          H       Me     H     T    CH    CH                                 COOMe      H       Me     H     T    CH    CH                                 CONH.sub.2 H       Me     H     T    CH    CH                                 CONHCOMe   H       Me     H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       Me     H     T    CH    CH                                 Ph         H       Me     H     T    CH    CH                                 Bz         H       Me     H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       Me     H     T    CH    CH                                 2-thienyl  H       Me     H     T    CH    CH                                 3-furyl    H       Me     H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       Me     H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       Me     H     T    CH    CH                                 T          H       Me     H     T    CH    CH                                 F          H       F      H     T    CH    CH                                 Cl         H       F      H     T    CH    CH                                 Br         H       F      H     T    CH    CH                                 I          H       F      H     T    CH    CH                                 Me         H       F      H     T    CH    CH                                 CF.sub.3   H       F      H     T    CH    CH                                 Et         H       F      H     T    CH    CH                                 n-Pr       H       F      H     T    CH    CH                                 c-Pr       H       F      H     T    CH    CH                                 NO.sub.2   H       F      H     T    CH    CH                                 NH.sub.2   H       F      H     T    CH    CH                                 N(Me)H     H       F      H     T    CH    CH                                 N(Me).sub.2                                                                              H       F      H     T    CH    CH                                 N(Me)n-Bu  H       F      H     T    CH    CH                                 N(nPen)H   H       F      H     T    CH    CH                                 NHCOPh     H       F      H     T    CH    CH                                 J.sup.1    H       F      H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       F      H     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       F      H     T    CH    CH                                 CHO        H       F      H     T    CH    CH                                 CN         H       F      H     T    CH    CH                                 U          H       F      H     T    CH    CH                                 COOMe      H       F      H     T    CH    CH                                 CONH.sub.2 H       F      H     T    CH    CH                                 CONHCOMe   H       F      H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       F      H     T    CH    CH                                 Ph         H       F      H     T    CH    CH                                 Bz         H       F      H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       F      H     T    CH    CH                                 2-thienyl  H       F      H     T    CH    CH                                 3-furyl    H       F      H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       F      H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       F      H     T    CH    CH                                 T          H       F      H     T    CH    CH                                 F          H       Cl     H     T    CH    CH                                 Cl         H       Cl     H     T    CH    CH                                 Br         H       Cl     H     T    CH    CH                                 I          H       Cl     H     T    CH    CH                                 Me         H       Cl     H     T    CH    CH                                 CF.sub.3   H       Cl     H     T    CH    CH                                 Et         H       Cl     H     T    CH    CH                                 n-Pr       H       Cl     H     T    CH    CH                                 c-Pr       H       Cl     H     T    CH    CH                                 NO.sub.2   H       Cl     H     T    CH    CH                                 NH.sub.2   H       Cl     H     T    CH    CH                                 N(Me)H     H       Cl     H     T    CH    CH                                 N(Me).sub.2                                                                              H       Cl     H     T    CH    CH                                 N(Me)n-Bu  H       Cl     H     T    CH    CH                                 N(nPen)H   H       Cl     H     T    CH    CH                                 NHCOPh     H       Cl     H     T    CH    CH                                 J.sup.1    H       Cl     H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       Cl     H     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       Cl     H     T    CH    CH                                 CHO        H       Cl     H     T    CH    CH                                 CN         H       Cl     H     T    CH    CH                                 U          H       Cl     H     T    CH    CH                                 COOMe      H       Cl     H     T    CH    CH                                 CONH.sub.2 H       Cl     H     T    CH    CH                                 CONHCOMe   H       Cl     H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       Cl     H     T    CH    CH                                 Ph         H       Cl     H     T    CH    CH                                 Bz         H       Cl     H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       Cl     H     T    CH    CH                                 2-thienyl  H       Cl     H     T    CH    CH                                 3-furyl    H       Cl     H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       Cl     H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       Cl     H     T    CH    CH                                 T          H       Cl     H     T    CH    CH                                 F          H       Br     H     T    CH    CH                                 Cl         H       Br     H     T    CH    CH                                 Br         H       Br     H     T    CH    CH                                 I          H       Br     H     T    CH    CH                                 Me         H       Br     H     T    CH    CH                                 CF.sub.3   H       Br     H     T    CH    CH                                 Et         H       Br     H     T    CH    CH                                 n-Pr       H       Br     H     T    CH    CH                                 c-Pr       H       Br     H     T    CH    CH                                 NO.sub.2   H       Br     H     T    CH    CH                                 NH.sub.2   H       Br     H     T    CH    CH                                 N(Me)H     H       Br     H     T    CH    CH                                 N(Me).sub.2                                                                              H       Br     H     T    CH    CH                                 N(Me)n-Bu  H       Br     H     T    CH    CH                                 N(nPen)H   H       Br     H     T    CH    CH                                 NHCOPh     H       Br     H     T    CH    CH                                 J.sup.1    H       Br     H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       Br     H     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       Br     H     T    CH    CH                                 CHO        H       Br     H     T    CH    CH                                 CN         H       Br     H     T    CH    CH                                 U          H       Br     H     T    CH    CH                                 COOMe      H       Br     H     T    CH    CH                                 CONH.sub.2 H       Br     H     T    CH    CH                                 CONHCOMe   H       Br     H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       Br     H     T    CH    CH                                 Ph         H       Br     H     T    CH    CH                                 Bz         H       Br     H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       Br     H     T    CH    CH                                 2-thienyl  H       Br     H     T    CH    CH                                 3-furyl    H       Br     H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       Br     H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       Br     H     T    CH    CH                                 T          H       Br     H     T    CH    CH                                 F          H       OH     H     T    CH    CH                                 Cl         H       OH     H     T    CH    CH                                 Br         H       OH     H     T    CH    CH                                 I          H       OH     H     T    CH    CH                                 Me         H       OH     H     T    CH    CH                                 CF.sub.3   H       OH     H     T    CH    CH                                 Et         H       OH     H     T    CH    CH                                 n-Pr       H       OH     H     T    CH    CH                                 c-Pr       H       OH     H     T    CH    CH                                 NO.sub.2   H       OH     H     T    CH    CH                                 NH.sub.2   H       OH     H     T    CH    CH                                 N(Me)H     H       OH     H     T    CH    CH                                 N(Me).sub.2                                                                              H       OH     H     T    CH    CH                                 N(Me)n-Bu  H       OH     H     T    CH    CH                                 N(nPen)H   H       OH     H     T    CH    CH                                 NHCOPh     H       OH     H     T    CH    CH                                 J.sup.1    H       OH     H     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       OH     H     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       OH     H     T    CH    CH                                 CHO        H       OH     H     T    CH    CH                                 CN         H       OH     H     T    CH    CH                                 U          H       OH     H     T    CH    CH                                 COOMe      H       OH     H     T    CH    CH                                 CONH.sub.2 H       OH     H     T    CH    CH                                 CONHCOMe   H       OH     H     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       OH     H     T    CH    CH                                 Ph         H       OH     H     T    CH    CH                                 Bz         H       OH     H     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       OH     H     T    CH    CH                                 2-thienyl  H       OH     H     T    CH    CH                                 3-furyl    H       OH     H     T    CH    CH                                 1-pyrrolyl H       OH     H     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       OH     H     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       OH     H     T    CH    CH                                 T          H       OH     H     T    CH    CH                                 F          H       H      Me    T    CH    CH                                 Cl         H       H      Me    T    CH    CH                                 Br         H       H      Me    T    CH    CH                                 I          H       H      Me    T    CH    CH                                 Me         H       H      Me    T    CH    CH                                 CF.sub.3   H       H      Me    T    CH    CH                                 Et         H       H      Me    T    CH    CH                                 n-Pr       H       H      Me    T    CH    CH                                 c-Pr       H       H      Me    T    CH    CH                                 NO.sub.2   H       H      Me    T    CH    CH                                 NH.sub.2   H       H      Me    T    CH    CH                                 N(Me)H     H       H      Me    T    CH    CH                                 N(Me).sub.2                                                                              H       H      Me    T    CH    CH                                 N(Me)n-Bu  H       H      Me    T    CH    CH                                 N(nPen)H   H       H      Me    T    CH    CH                                 NHCOPh     H       H      Me    T    CH    CH                                 J.sup.1    H       H      Me    T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       H      Me    T    CH    CH                                 C(NH)NH.sub.2                                                                            H       H      Me    T    CH    CH                                 CHO        H       H      Me    T    CH    CH                                 CN         H       H      Me    T    CH    CH                                 U          H       H      Me    T    CH    CH                                 COOMe      H       H      Me    T    CH    CH                                 CONH.sub.2 H       H      Me    T    CH    CH                                 CONHCOMe   H       H      Me    T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      Me    T    CH    CH                                 Ph         H       H      Me    T    CH    CH                                 Bz         H       H      Me    T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      Me    T    CH    CH                                 2-thienyl  H       H      Me    T    CH    CH                                 3-furyl    H       H      Me    T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       H      Me    T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      Me    T    CH    CH                                 T          H       H      Me    T    CH    CH                                 F          H       H      F     T    CH    CH                                 Cl         H       H      F     T    CH    CH                                 Br         H       H      F     T    CH    CH                                 I          H       H      F     T    CH    CH                                 Me         H       H      F     T    CH    CH                                 CF.sub.3   H       H      F     T    CH    CH                                 Et         H       H      F     T    CH    CH                                 n-Pr       H       H      F     T    CH    CH                                 c-Pr       H       H      F     T    CH    CH                                 NO.sub.2   H       H      F     T    CH    CH                                 NH.sub.2   H       H      F     T    CH    CH                                 N(Me)H     H       H      F     T    CH    CH                                 N(Me).sub.2                                                                              H       H      F     T    CH    CH                                 N(Me)n-Bu  H       H      F     T    CH    CH                                 N(nPen)H   H       H      F     T    CH    CH                                 NHCOPh     H       H      F     T    CH    CH                                 J.sup.1    H       H      F     T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       H      F     T    CH    CH                                 C(NH)NH.sub.2                                                                            H       H      F     T    CH    CH                                 CHO        H       H      F     T    CH    CH                                 CN         H       H      F     T    CH    CH                                 U          H       H      F     T    CH    CH                                 COOMe      H       H      F     T    CH    CH                                 CONH.sub.2 H       H      F     T    CH    CH                                 CONHCOMe   H       H      F     T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      F     T    CH    CH                                 Ph         H       H      F     T    CH    CH                                 Bz         H       H      F     T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      F     T    CH    CH                                 2-thienyl  H       H      F     T    CH    CH                                 3-furyl    H       H      F     T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       H      F     T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      F     T    CH    CH                                 T          H       H      F     T    CH    CH                                 F          H       H      Cl    T    CH    CH                                 Cl         H       H      Cl    T    CH    CH                                 Br         H       H      Cl    T    CH    CH                                 I          H       H      Cl    T    CH    CH                                 Me         H       H      Cl    T    CH    CH                                 CF.sub.3   H       H      Cl    T    CH    CH                                 Et         H       H      Cl    T    CH    CH                                 n-Pr       H       H      Cl    T    CH    CH                                 c-Pr       H       H      Cl    T    CH    CH                                 NO.sub.2   H       H      Cl    T    CH    CH                                 NH.sub.2   H       H      Cl    T    CH    CH                                 N(Me)H     H       H      Cl    T    CH    CH                                 N(Me).sub.2                                                                              H       H      Cl    T    CH    CH                                 N(Me)n-Bu  H       H      Cl    T    CH    CH                                 N(nPen)H   H       H      Cl    T    CH    CH                                 NHCOPh     H       H      Cl    T    CH    CH                                 J.sup.1    H       H      Cl    T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       H      Cl    T    CH    CH                                 C(NH)NH.sub.2                                                                            H       H      Cl    T    CH    CH                                 CHO        H       H      Cl    T    CH    CH                                 CN         H       H      Cl    T    CH    CH                                 U          H       H      Cl    T    CH    CH                                 COOMe      H       H      Cl    T    CH    CH                                 CONH.sub.2 H       H      Cl    T    CH    CH                                 CONHCOMe   H       H      Cl    T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      Cl    T    CH    CH                                 Ph         H       H      Cl    T    CH    CH                                 Bz         H       H      Cl    T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      Cl    T    CH    CH                                 2-thienyl  H       H      Cl    T    CH    CH                                 3-furyl    H       H      Cl    T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       H      Cl    T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      Cl    T    CH    CH                                 T          H       H      Cl    T    CH    CH                                 F          H       H      Br    T    CH    CH                                 Cl         H       H      Br    T    CH    CH                                 Br         H       H      Br    T    CH    CH                                 I          H       H      Br    T    CH    CH                                 Me         H       H      Br    T    CH    CH                                 CF.sub.3   H       H      Br    T    CH    CH                                 Et         H       H      Br    T    CH    CH                                 n-Pr       H       H      Br    T    CH    CH                                 c-Pr       H       H      Br    T    CH    CH                                 NO.sub.2   H       H      Br    T    CH    CH                                 NH.sub.2   H       H      Br    T    CH    CH                                 N(Me)H     H       H      Br    T    CH    CH                                 N(Me).sub.2                                                                              H       H      Br    T    CH    CH                                 N(Me)n-Bu  H       H      Br    T    CH    CH                                 N(nPen)H   H       H      Br    T    CH    CH                                 NHCOPh     H       H      Br    T    CH    CH                                 J.sup.1    H       H      Br    T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       H      Br    T    CH    CH                                 C(NH)NH.sub.2                                                                            H       H      Br    T    CH    CH                                 CHO        H       H      Br    T    CH    CH                                 CN         H       H      Br    T    CH    CH                                 U          H       H      Br    T    CH    CH                                 COOMe      H       H      Br    T    CH    CH                                 CONH.sub.2 H       H      Br    T    CH    CH                                 CONHCOMe   H       H      Br    T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      Br    T    CH    CH                                 Ph         H       H      Br    T    CH    CH                                 Bz         H       H      Br    T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      Br    T    CH    CH                                 2-thienyl  H       H      Br    T    CH    CH                                 3-furyl    H       H      Br    T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       H      Br    T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      Br    T    CH    CH                                 T          H       H      Br    T    CH    CH                                 F          H       H      OH    T    CH    CH                                 Cl         H       H      OH    T    CH    CH                                 Br         H       H      OH    T    CH    CH                                 I          H       H      OH    T    CH    CH                                 Me         H       H      OH    T    CH    CH                                 CF.sub.3   H       H      OH    T    CH    CH                                 Et         H       H      OH    T    CH    CH                                 n-Pr       H       H      OH    T    CH    CH                                 c-Pr       H       H      OH    T    CH    CH                                 NO.sub.2   H       H      OH    T    CH    CH                                 NH.sub.2   H       H      OH    T    CH    CH                                 N(Me)H     H       H      OH    T    CH    CH                                 N(Me).sub.2                                                                              H       H      OH    T    CH    CH                                 N(Me)n-Bu  H       H      OH    T    CH    CH                                 N(nPen)H   H       H      OH    T    CH    CH                                 NHCOPh     H       H      OH    T    CH    CH                                 J.sup.1    H       H      OH    T    CH    CH                                 NHC(NH)NH.sub.2                                                                          H       H      OH    T    CH    CH                                 C(NH)NH.sub.2                                                                            H       H      OH    T    CH    CH                                 CHO        H       H      OH    T    CH    CH                                 CN         H       H      OH    T    CH    CH                                 U          H       H      OH    T    CH    CH                                 COOMe      H       H      OH    T    CH    CH                                 CONH.sub.2 H       H      OH    T    CH    CH                                 CONHCOMe   H       H      OH    T    CH    CH                                 CH.sub.2 N(nPen)COPh                                                                     H       H      OH    T    CH    CH                                 Ph         H       H      OH    T    CH    CH                                 Bz         H       H      OH    T    CH    CH                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      OH    T    CH    CH                                 2-thienyl  H       H      OH    T    CH    CH                                 3-furyl    H       H      OH    T    CH    CH                                 Ph(4-J.sup.2)                                                                            H       H      OH    T    CH    CH                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      OH    T    CH    CH                                 T          H       H      OH    T    CH    CH                                 F          H       H      H     T    CH    CMe                                Cl         H       H      H     T    CH    CMe                                Br         H       H      H     T    CH    CMe                                I          H       H      H     T    CH    CMe                                Me         H       H      H     T    CH    CMe                                CF.sub.3   H       H      H     T    CH    CMe                                Et         H       H      H     T    CH    CMe                                n-Pr       H       H      H     T    CH    CMe                                c-Pr       H       H      H     T    CH    CMe                                NO.sub.2   H       H      H     T    CH    CMe                                NH.sub.2   H       H      H     T    CH    CMe                                N(Me)H     H       H      H     T    CH    CMe                                N(Me).sub.2                                                                              H       H      H     T    CH    CMe                                N(Me)n-Bu  H       H      H     T    CH    CMe                                N(nPen)H   H       H      H     T    CH    CMe                                NHCOPh     H       H      H     T    CH    CMe                                J.sup.1    H       H      H     T    CH    CMe                                NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    CMe                                C(NH)NH.sub.2                                                                            H       H      H     T    CH    CMe                                CHO        H       H      H     T    CH    CMe                                CN         H       H      H     T    CH    CMe                                U          H       H      H     T    CH    CMe                                COOMe      H       H      H     T    CH    CMe                                CONH.sub.2 H       H      H     T    CH    CMe                                CONHCOMe   H       H      H     T    CH    CMe                                CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    CMe                                Ph         H       H      H     T    CH    CMe                                Bz         H       H      H     T    CH    CMe                                CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    CMe                                2-thienyl  H       H      H     T    CH    CMe                                3-furyl    H       H      H     T    CH    CMe                                Ph(4-J.sup.2)                                                                            H       H      H     T    CH    CMe                                Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    CMe                                T          H       H      H     T    CH    CMe                                F          H       H      H     T    CH    CF                                 Cl         H       H      H     T    CH    CF                                 Br         H       H      H     T    CH    CF                                 I          H       H      H     T    CH    CF                                 Me         H       H      H     T    CH    CF                                 CF.sub.3   H       H      H     T    CH    CF                                 Et         H       H      H     T    CH    CF                                 n-Pr       H       H      H     T    CH    CF                                 c-Pr       H       H      H     T    CH    CF                                 NO.sub.2   H       H      H     T    CH    CF                                 NH.sub.2   H       H      H     T    CH    CF                                 N(Me)H     H       H      H     T    CH    CF                                 N(Me).sub.2                                                                              H       H      H     T    CH    CF                                 N(Me)n-Bu  H       H      H     T    CH    CF                                 N(nPen)H   H       H      H     T    CH    CF                                 NHCOPh     H       H      H     T    CH    CF                                 J.sup.1    H       H      H     T    CH    CF                                 NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    CF                                 C(NH)NH.sub.2                                                                            H       H      H     T    CH    CF                                 CHO        H       H      H     T    CH    CF                                 CN         H       H      H     T    CH    CF                                 U          H       H      H     T    CH    CF                                 COOMe      H       H      H     T    CH    CF                                 CONH.sub.2 H       H      H     T    CH    CF                                 CONHCOMe   H       H      H     T    CH    CF                                 CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    CF                                 Ph         H       H      H     T    CH    CF                                 Bz         H       H      H     T    CH    CF                                 CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    CF                                 2-thienyl  H       H      H     T    CH    CF                                 3-furyl    H       H      H     T    CH    CF                                 Ph(4-J.sup.2)                                                                            H       H      H     T    CH    CF                                 Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    CF                                 T          H       H      H     T    CH    CF                                 F          H       H      H     T    CH    CCl                                Cl         H       H      H     T    CH    CCl                                Br         H       H      H     T    CH    CCl                                I          H       H      H     T    CH    CCl                                Me         H       H      H     T    CH    CCl                                CF.sub.3   H       H      H     T    CH    CCl                                Et         H       H      H     T    CH    CCl                                n-Pr       H       H      H     T    CH    CCl                                c-Pr       H       H      H     T    CH    CCl                                NO.sub.2   H       H      H     T    CH    CCl                                NH.sub.2   H       H      H     T    CH    CCl                                N(Me)H     H       H      H     T    CH    CCl                                N(Me).sub.2                                                                              H       H      H     T    CH    CCl                                N(Me)n-Bu  H       H      H     T    CH    CCl                                N(nPen)H   H       H      H     T    CH    CCl                                NHCOPh     H       H      H     T    CH    CCl                                J.sup.1    H       H      H     T    CH    CCl                                NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    CCl                                C(NH)NH.sub.2                                                                            H       H      H     T    CH    CCl                                CHO        H       H      H     T    CH    CCl                                CN         H       H      H     T    CH    CCl                                U          H       H      H     T    CH    CCl                                COOMe      H       H      H     T    CH    CCl                                CONH.sub.2 H       H      H     T    CH    CCl                                CONHCOMe   H       H      H     T    CH    CCl                                CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    CCl                                Ph         H       H      H     T    CH    CCl                                Bz         H       H      H     T    CH    CCl                                CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    CCl                                2-thienyl  H       H      H     T    CH    CCl                                3-furyl    H       H      H     T    CH    CCl                                Ph(4-J.sup.2)                                                                            H       H      H     T    CH    CCl                                Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    CCl                                T          H       H      H     T    CH    CCl                                F          H       H      H     T    CH    CBr                                Cl         H       H      H     T    CH    CBr                                Br         H       H      H     T    CH    CBr                                I          H       H      H     T    CH    CBr                                Me         H       H      H     T    CH    CBr                                CF.sub.3   H       H      H     T    CH    CBr                                Et         H       H      H     T    CH    CBr                                n-Pr       H       H      H     T    CH    CBr                                c-Pr       H       H      H     T    CH    CBr                                NO.sub.2   H       H      H     T    CH    CBr                                NH.sub.2   H       H      H     T    CH    CBr                                N(Me)H     H       H      H     T    CH    CBr                                N(Me).sub.2                                                                              H       H      H     T    CH    CBr                                N(Me)n-Bu  H       H      H     T    CH    CBr                                N(nPen)H   H       H      H     T    CH    CBr                                NHCOPh     H       H      H     T    CH    CBr                                J.sup.1    H       H      H     T    CH    CBr                                NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    CBr                                C(NH)NH.sub.2                                                                            H       H      H     T    CH    CBr                                CHO        H       H      H     T    CH    CBr                                CN         H       H      H     T    CH    CBr                                U          H       H      H     T    CH    CBr                                COOMe      H       H      H     T    CH    CBr                                CONH.sub.2 H       H      H     T    CH    CBr                                CONHCOMe   H       H      H     T    CH    CBr                                CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    CBr                                Ph         H       H      H     T    CH    CBr                                Bz         H       H      H     T    CH    CBr                                CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    CBr                                2-thienyl  H       H      H     T    CH    CBr                                3-furyl    H       H      H     T    CH    CBr                                Ph(4-J.sup.2)                                                                            H       H      H     T    CH    CBr                                Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    CBr                                T          H       H      H     T    CH    CBr                                F          H       H      H     T    CH    COH                                Cl         H       H      H     T    CH    COH                                Br         H       H      H     T    CH    COH                                I          H       H      H     T    CH    COH                                Me         H       H      H     T    CH    COH                                CF.sub.3   H       H      H     T    CH    COH                                Et         H       H      H     T    CH    COH                                n-Pr       H       H      H     T    CH    COH                                c-Pr       H       H      H     T    CH    COH                                NO.sub.2   H       H      H     T    CH    COH                                NH.sub.2   H       H      H     T    CH    COH                                N(Me)H     H       H      H     T    CH    COH                                N(Me).sub.2                                                                              H       H      H     T    CH    COH                                N(Me)n-Bu  H       H      H     T    CH    COH                                N(nPen)H   H       H      H     T    CH    COH                                NHCOPh     H       H      H     T    CH    COH                                J.sup.1    H       H      H     T    CH    COH                                NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    COH                                C(NH)NH.sub.2                                                                            H       H      H     T    CH    COH                                CHO        H       H      H     T    CH    COH                                CN         H       H      H     T    CH    COH                                U          H       H      H     T    CH    COH                                COOMe      H       H      H     T    CH    COH                                CONH.sub.2 H       H      H     T    CH    COH                                CONHCOMe   H       H      H     T    CH    COH                                CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    COH                                Ph         H       H      H     T    CH    COH                                Bz         H       H      H     T    CH    COH                                CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    COH                                2-thienyl  H       H      H     T    CH    COH                                3-furyl    H       H      H     T    CH    COH                                Ph(4-J.sup.2)                                                                            H       H      H     T    CH    COH                                Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    COH                                T          H       H      H     T    CH    COH                                F          H       H      H     T    CH    N                                  Cl         H       H      H     T    CH    N                                  Br         H       H      H     T    CH    N                                  I          H       H      H     T    CH    N                                  Me         H       H      H     T    CH    N                                  CF.sub.3   H       H      H     T    CH    N                                  Et         H       H      H     T    CH    N                                  n-Pr       H       H      H     T    CH    N                                  c-Pr       H       H      H     T    CH    N                                  NO.sub.2   H       H      H     T    CH    N                                  NH.sub.2   H       H      H     T    CH    N                                  N(Me)H     H       H      H     T    CH    N                                  N(Me).sub.2                                                                              H       H      H     T    CH    N                                  N(Me)n-Bu  H       H      H     T    CH    N                                  N(nPen)H   H       H      H     T    CH    N                                  NHCOPh     H       H      H     T    CH    N                                  J.sup.1    H       H      H     T    CH    N                                  NHC(NH)NH.sub.2                                                                          H       H      H     T    CH    N                                  C(NH)NH.sub.2                                                                            H       H      H     T    CH    N                                  CHO        H       H      H     T    CH    N                                  CN         H       H      H     T    CH    N                                  U          H       H      H     T    CH    N                                  COOMe      H       H      H     T    CH    N                                  CONH.sub.2 H       H      H     T    CH    N                                  CONHCOMe   H       H      H     T    CH    N                                  CH.sub.2 N(nPen)COPh                                                                     H       H      H     T    CH    N                                  Ph         H       H      H     T    CH    N                                  Bz         H       H      H     T    CH    N                                  CH.sub.2 CH.sub.2 Ph                                                                     H       H      H     T    CH    N                                  2-thienyl  H       H      H     T    CH    N                                  3-furyl    H       H      H     T    CH    N                                  Ph(4-J.sup.2)                                                                            H       H      H     T    CH    N                                  Ph(2-Cl, 5-J.sup.1)                                                                      H       H      H     T    CH    N                                  T          H       H      H     T    CH    N                                  ______________________________________                                    

                                      TABLE 3                                     __________________________________________________________________________     ##STR28##                                                                    R.sup.3    R.sup.60                                                                            R.sup.61                                                                           R.sup.62                                                                            R.sup.63                                                                           R.sup.64                                     __________________________________________________________________________    F          Me    H    H     H    H                                            Cl         Me    H    H     H    H                                            Br         Me    H    H     H    H                                            I          Me    H    H     H    H                                            Me         Me    H    H     H    H                                            CF.sub.3   Me    H    H     H    H                                            Et         Me    H    H     H    H                                            n-Pr       Me    H    H     H    H                                            c-Pr       Me    H    H     H    H                                            NO.sub.2   Me    H    H     H    H                                            NH.sub.2   Me    H    H     H    H                                            N(Me)n-Bu  Me    H    H     H    H                                            N(nPen)H   Me    H    H     H    H                                            NHCOPh     Me    H    H     H    H                                            J.sup.1    Me    H    H     H    H                                            U          Me    H    H     H    H                                            COOMe      Me    H    H     H    H                                            CONH.sub.2 Me    H    H     H    H                                            CONHCOMe   Me    H    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     Me    H    H     H    H                                            Ph         Me    H    H     H    H                                            Bz         Me    H    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     Me    H    H     H    H                                            2-thienyl  Me    H    H     H    H                                            3-furyl    Me    H    H     H    H                                            Ph(4-J.sup.2)                                                                            Me    H    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Me    H    H     H    H                                            T          Me    H    H     H    H                                            F          H     Me   H     H    H                                            Cl         H     Me   H     H    H                                            Br         H     Me   H     H    H                                            I          H     Me   H     H    H                                            Me         H     Me   H     H    H                                            CF.sub.3   H     Me   H     H    H                                            Et         H     Me   H     H    H                                            n-Pr       H     Me   H     H    H                                            c-Pr       H     Me   H     H    H                                            NO.sub.2   H     Me   H     H    H                                            NH.sub.2   H     Me   H     H    H                                            N(Me)n-Bu  H     Me   H     H    H                                            N(nPen)H   H     Me   H     H    H                                            NHCOPh     H     Me   H     H    H                                            J.sup.1    H     Me   H     H    H                                            U          H     Me   H     H    H                                            COOMe      H     Me   H     H    H                                            CONH.sub.2 H     Me   H     H    H                                            CONHCOMe   H     Me   H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     Me   H     H    H                                            Ph         H     Me   H     H    H                                            Bz         H     Me   H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     Me   H     H    H                                            2-thienyl  H     Me   H     H    H                                            3-furyl    H     Me   H     H    H                                            Ph(4-J.sup.2)                                                                            H     Me   H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     Me   H     H    H                                            T          H     Me   H     H    H                                            F          H     H    Me    H    H                                            Cl         H     H    Me    H    H                                            Br         H     H    Me    H    H                                            I          H     H    Me    H    H                                            Me         H     H    Me    H    H                                            CF.sub.3   H     H    Me    H    H                                            Et         H     H    Me    H    H                                            n-Pr       H     H    Me    H    H                                            c-Pr       H     H    Me    H    H                                            NO.sub.2   H     H    Me    H    H                                            NH.sub.2   H     H    Me    H    H                                            N(nPen)H   H     H    Me    H    H                                            NHCOPh     H     H    Me    H    H                                            J.sup.1    H     H    Me    H    H                                            U          H     H    Me    H    H                                            COOMe      H     H    Me    H    H                                            CONH.sub.2 H     H    Me    H    H                                            CONHCOMe   H     H    Me    H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     H    Me    H    H                                            Ph         H     H    Me    H    H                                            Bz         H     H    Me    H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     H    Me    H    H                                            2-thienyl  H     H    Me    H    H                                            3-furyl    H     H    Me    H    H                                            Ph(4-J.sup.2)                                                                            H     H    Me    H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     H    Me    H    H                                            T          H     H    Me    H    H                                            F          F     H    H     H    H                                            Cl         F     H    H     H    H                                            Br         F     H    H     H    H                                            I          F     H    H     H    H                                            Me         F     H    H     H    H                                            CF.sub.3   F     H    H     H    H                                            Et         F     H    H     H    H                                            n-Pr       F     H    H     H    H                                            c-Pr       F     H    H     H    H                                            NO.sub.2   F     H    H     H    H                                            NH.sub.2   F     H    H     H    H                                            N(Me)n-Bu  F     H    H     H    H                                            N(nPen)H   F     H    H     H    H                                            NHCOPh     F     H    H     H    H                                            J.sup.1    F     H    H     H    H                                            U          F     H    H     H    H                                            COOMe      F     H    H     H    H                                            CONH.sub.2 F     H    H     H    H                                            CONHCOMe   F     H    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     F     H    H     H    H                                            Ph         F     H    H     H    H                                            Bz         F     H    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     F     H    H     H    H                                            2-thienyl  F     H    H     H    H                                            3-furyl    F     H    H     H    H                                            Ph(4-J.sup.2)                                                                            F     H    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      F     H    H     H    H                                            T          F     H    H     H    H                                            F          H     F    H     H    H                                            Cl         H     F    H     H    H                                            Br         H     F    H     H    H                                            I          H     F    H     H    H                                            Me         H     F    H     H    H                                            CF.sub.3   H     F    H     H    H                                            Et         H     F    H     H    H                                            n-Pr       H     F    H     H    H                                            c-Pr       H     F    H     H    H                                            NO.sub.2   H     F    H     H    H                                            N(Me)n-Bu  H     F    H     H    H                                            N(nPen)H   H     F    H     H    H                                            NHCOPh     H     F    H     H    H                                            J.sup.1    H     F    H     H    H                                            U          H     F    H     H    H                                            COOMe      H     F    H     H    H                                            CONH.sub.2 H     F    H     H    H                                            CONHCOMe   H     F    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     F    H     H    H                                            Ph         H     F    H     H    H                                            Bz         H     F    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     F    H     H    H                                            2-thienyl  H     F    H     H    H                                            3-furyl    H     F    H     H    H                                            Ph(4-J.sup.2)                                                                            H     F    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     F    H     H    H                                            T          H     F    H     H    H                                            F          H     H    F     H    H                                            Cl         H     H    F     H    H                                            Br         H     H    F     H    H                                            I          H     H    F     H    H                                            Me         H     H    F     H    H                                            CF.sub.3   H     H    F     H    H                                            Et         H     H    F     H    H                                            n-Pr       H     H    F     H    H                                            c-Pr       H     H    F     H    H                                            NO.sub.2   H     H    F     H    H                                            NH.sub.2   H     H    F     H    H                                            N(Me)n-Bu  H     H    F     H    H                                            N(nPen)H   H     H    F     H    H                                            NHCOPh     H     H    F     H    H                                            J.sup.1    H     H    F     H    H                                            U          H     H    F     H    H                                            COOMe      H     H    F     H    H                                            CONH.sub.2 H     H    F     H    H                                            CONHCOMe   H     H    F     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     H    F     H    H                                            Ph         H     H    F     H    H                                            Bz         H     H    F     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     H    F     H    H                                            2-thienyl  H     H    F     H    H                                            3-furyl    H     H    F     H    H                                            Ph(4-J.sup.2)                                                                            H     H    F     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     H    F     H    H                                            T          H     H    F     H    H                                            F          Cl    H    H     H    H                                            Cl         Cl    H    H     H    H                                            Br         Cl    H    H     H    H                                            I          Cl    H    H     H    H                                            Me         Cl    H    H     H    H                                            CF.sub.3   Cl    H    H     H    H                                            Et         Cl    H    H     H    H                                            n-Pr       Cl    H    H     H    H                                            c-Pr       Cl    H    H     H    H                                            NO.sub.2   Cl    H    H     H    H                                            NH.sub.2   Cl    H    H     H    H                                            N(Me)n-Bu  Cl    H    H     H    H                                            N(nPen)H   Cl    H    H     H    H                                            NHCOPh     Cl    H    H     H    H                                            J.sup.1    Cl    H    H     H    H                                            U          Cl    H    H     H    H                                            COOMe      Cl    H    H     H    H                                            CONH.sub.2 Cl    H    H     H    H                                            CONHCOMe   Cl    H    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     Cl    H    H     H    H                                            Ph         Cl    H    H     H    H                                            Bz         Cl    H    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     Cl    H    H     H    H                                            2-thienyl  Cl    H    H     H    H                                            3-furyl    Cl    H    H     H    H                                            Ph(4-J.sup.2)                                                                            Cl    H    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Cl    H    H     H    H                                            T          Cl    H    H     H    H                                            F          H     Cl   H     H    H                                            Cl         H     Cl   H     H    H                                            Br         H     Cl   H     H    H                                            I          H     Cl   H     H    H                                            Me         H     Cl   H     H    H                                            CF.sub.3   H     Cl   H     H    H                                            Et         H     Cl   H     H    H                                            n-Pr       H     Cl   H     H    H                                            c-Pr       H     Cl   H     H    H                                            NO.sub.2   H     Cl   H     H    H                                            NH.sub.2   H     Cl   H     H    H                                            N(Me)n-Bu  H     Cl   H     H    H                                            N(nPen)H   H     Cl   H     H    H                                            NHCOPh     H     Cl   H     H    H                                            J.sup.1    H     Cl   H     H    H                                            U          H     Cl   H     H    H                                            COOMe      H     Cl   H     H    H                                            CONH.sub.2 H     Cl   H     H    H                                            CONHCOMe   H     Cl   H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     Cl   H     H    H                                            Ph         H     Cl   H     H    H                                            Bz         H     Cl   H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     Cl   H     H    H                                            2-thienyl  H     Cl   H     H    H                                            3-furyl    H     Cl   H     H    H                                            Ph(4-J.sup.2)                                                                            H     Cl   H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     Cl   H     H    H                                            T          H     Cl   H     H    H                                            F          H     H    Cl    H    H                                            Cl         H     H    Cl    H    H                                            Br         H     H    Cl    H    H                                            I          H     H    Cl    H    H                                            Me         H     H    Cl    H    H                                            CF.sub.3   H     H    Cl    H    H                                            Et         H     H    Cl    H    H                                            n-Pr       H     H    Cl    H    H                                            c-Pr       H     H    Cl    H    H                                            NO.sub.2   H     H    Cl    H    H                                            NH.sub.2   H     H    Cl    H    H                                            N(Me)n-Bu  H     H    Cl    H    H                                            N(nPen)H   H     H    Cl    H    H                                            NHCOPh     H     H    Cl    H    H                                            J.sup.1    H     H    Cl    H    H                                            U          H     H    Cl    H    H                                            COOMe      H     H    Cl    H    H                                            CONH.sub.2 H     H    Cl    H    H                                            CONHCOMe   H     H    Cl    H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     H    Cl    H    H                                            Ph         H     H    Cl    H    H                                            Bz         H     H    Cl    H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     H    Cl    H    H                                            2-thienyl  H     H    Cl    H    H                                            3-furyl    H     H    Cl    H    H                                            Ph(4-J.sup.2)                                                                            H     H    Cl    H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     H    Cl    H    H                                            T          H     H    Cl    H    H                                            F          Br    H    H     H    H                                            Cl         Br    H    H     H    H                                            Br         Br    H    H     H    H                                            I          Br    H    H     H    H                                            Me         Br    H    H     H    H                                            CF.sub.3   Br    H    H     H    H                                            Et         Br    H    H     H    H                                            n-Pr       Br    H    H     H    H                                            c-Pr       Br    H    H     H    H                                            NO.sub.2   Br    H    H     H    H                                            NH.sub.2   Br    H    H     H    H                                            N(Me)n-Bu  Br    H    H     H    H                                            N(nPen)H   Br    H    H     H    H                                            NHCOPh     Br    H    H     H    H                                            N(Me)CONHPh                                                                              Br    H    H     H    H                                            J.sup.1    Br    H    H     H    H                                            U          Br    H    H     H    H                                            COOMe      Br    H    H     H    H                                            CONH.sub.2 Br    H    H     H    H                                            CONHCOMe   Br    H    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     Br    H    H     H    H                                            Ph         Br    H    H     H    H                                            Bz         Br    H    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     Br    H    H     H    H                                            2-thienyl  Br    H    H     H    H                                            3-furyl    Br    H    H     H    H                                            Ph(4-J.sup.2)                                                                            Br    H    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Br    H    H     H    H                                            T          Br    H    H     H    H                                            F          H     Br   H     H    H                                            Cl         H     Br   H     H    H                                            Br         H     Br   H     H    H                                            I          H     Br   H     H    H                                            Me         H     Br   H     H    H                                            CF.sub.3   H     Br   H     H    H                                            Et         H     Br   H     H    H                                            n-Pr       H     Br   H     H    H                                            c-Pr       H     Br   H     H    H                                            NO.sub.2   H     Br   H     H    H                                            NH.sub.2   H     Br   H     H    H                                            N(Me)n-Bu  H     Br   H     H    H                                            N(nPen)H   H     Br   H     H    H                                            NHCOPh     H     Br   H     H    H                                            J.sup.1    H     Br   H     H    H                                            U          H     Br   H     H    H                                            COOMe      H     Br   H     H    H                                            CONH.sub.2 H     Br   H     H    H                                            CONHCOMe   H     Br   H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     Br   H     H    H                                            Ph         H     Br   H     H    H                                            Bz         H     Br   H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     Br   H     H    H                                            2-thienyl  H     Br   H     H    H                                            3-furyl    H     Br   H     H    H                                            Ph(4-J.sup.2)                                                                            H     Br   H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     Br   H     H    H                                            T          H     Br   H     H    H                                            F          H     Br   H     H    H                                            Cl         H     Br   H     H    H                                            Br         H     Br   H     H    H                                            I          H     H    Br    H    H                                            Me         H     H    Br    H    H                                            CF.sub.3   H     H    Br    H    H                                            Et         H     H    Br    H    H                                            n-Pr       H     H    Br    H    H                                            c-Pr       H     H    Br    H    H                                            NO.sub.2   H     H    Br    H    H                                            N(Me)n-Bu  H     H    Br    H    H                                            N(nPen)H   H     H    Br    H    H                                            NHCOPh     H     H    Br    H    H                                            J.sup.1    H     H    Br    H    H                                            U          H     H    Br    H    H                                            COOMe      H     H    Br    H    H                                            CONH.sub.2 H     H    Br    H    H                                            CONHCOMe   H     H    Br    H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     H    Br    H    H                                            Ph         H     H    Br    H    H                                            Bz         H     H    Br    H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     H    Br    H    H                                            2-thienyl  H     H    Br    H    H                                            3-furyl    H     H    Br    H    H                                            Ph(4-J.sup.2)                                                                            H     H    Br    H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     H    Br    H    H                                            T          H     H    Br    H    H                                            F          J.sup.2                                                                             H    H     H    H                                            Cl         J.sup.2                                                                             H    H     H    H                                            Br         J.sup.2                                                                             H    H     H    H                                            I          J.sup.2                                                                             H    H     H    H                                            Me         J.sup.2                                                                             H    H     H    H                                            CF.sub.3   J.sup.2                                                                             H    H     H    H                                            Et         J.sup.2                                                                             H    H     H    H                                            n-Pr       J.sup.2                                                                             H    H     H    H                                            c-Pr       J.sup.2                                                                             H    H     H    H                                            NO.sub.2   J.sup.2                                                                             H    H     H    H                                            NH.sub.2   J.sup.2                                                                             H    H     H    H                                            N(Me)n-Bu  J.sup.2                                                                             H    H     H    H                                            N(nPen)H   J.sup.2                                                                             H    H     H    H                                            NHCOPh     J.sup.2                                                                             H    H     H    H                                            J.sup.1    J.sup.2                                                                             H    H     H    H                                            U          J.sup.2                                                                             H    H     H    H                                            COOMe      J.sup.2                                                                             H    H     H    H                                            CONH.sub.2 J.sup.2                                                                             H    H     H    H                                            CONHCOMe   J.sup.2                                                                             H    H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     J.sup.2                                                                             H    H     H    H                                            Ph         J.sup.2                                                                             H    H     H    H                                            Bz         J.sup.2                                                                             H    H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     J.sup.2                                                                             H    H     H    H                                            2-thienyl  J.sup.2                                                                             H    H     H    H                                            3-furyl    J.sup.2                                                                             H    H     H    H                                            Ph(4-J.sup.2)                                                                            J.sup.2                                                                             H    H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      J.sup.2                                                                             H    H     H    H                                            T          J.sup.2                                                                             H    H     H    H                                            F          H     J.sup.2                                                                            H     H    H                                            Cl         H     J.sup.2                                                                            H     H    H                                            Br         H     J.sup.2                                                                            H     H    H                                            I          H     J.sup.2                                                                            H     H    H                                            Me         H     J.sup.2                                                                            H     H    H                                            CF.sub.3   H     J.sup.2                                                                            H     H    H                                            Et         H     J.sup.2                                                                            H     H    H                                            n-Pr       H     J.sup.2                                                                            H     H    H                                            c-Pr       H     J.sup.2                                                                            H     H    H                                            NO.sub.2   H     J.sup.2                                                                            H     H    H                                            NH.sub.2   H     J.sup.2                                                                            H     H    H                                            N(Me)n-Bu  H     J.sup.2                                                                            H     H    H                                            N(nPen)H   H     J.sup.2                                                                            H     H    H                                            NHCOPh     H     J.sup.2                                                                            H     H    H                                            J.sup.1    H     J.sup.2                                                                            H     H    H                                            U          H     J.sup.2                                                                            H     H    H                                            COOMe      H     J.sup.2                                                                            H     H    H                                            CONH.sub.2 H     J.sup.2                                                                            H     H    H                                            CONHCOMe   H     J.sup.2                                                                            H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     J.sup.2                                                                            H     H    H                                            Ph         H     J.sup.2                                                                            H     H    H                                            Bz         H     J.sup.2                                                                            H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     J.sup.2                                                                            H     H    H                                            2-thienyl  H     J.sup.2                                                                            H     H    H                                            3-furyl    H     J.sup.2                                                                            H     H    H                                            Ph(4-J.sup.2)                                                                            H     J.sup.2                                                                            H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     J.sup.2                                                                            H     H    H                                            T          H     H    J.sup.2                                                                             H    H                                            F          H     H    J.sup.2                                                                             H    H                                            Cl         H     H    J.sup.2                                                                             H    H                                            Br         H     H    J.sup.2                                                                             H    H                                            I          H     H    J.sup.2                                                                             H    H                                            Me         H     H    J.sup.2                                                                             H    H                                            CF.sub.3   H     H    J.sup.2                                                                             H    H                                            Et         H     H    J.sup.2                                                                             H    H                                            n-Pr       H     H    J.sup.2                                                                             H    H                                            c-Pr       H     H    J.sup.2                                                                             H    H                                            NO.sub.2   H     H    J.sup.2                                                                             H    H                                            NH.sub.2   H     H    J.sup.2                                                                             H    H                                            N(Me)n-Bu  H     H    J.sup.2                                                                             H    H                                            N(nPen)H   H     H    J.sup.2                                                                             H    H                                            NHCOPh     H     H    J.sup.2                                                                             H    H                                            J.sup.1    H     H    J.sup.2                                                                             H    H                                            U          H     H    J.sup.2                                                                             H    H                                            COOMe      H     H    J.sup.2                                                                             H    H                                            CONH.sub.2 H     H    J.sup.2                                                                             H    H                                            CONHCOMe   H     H    J.sup.2                                                                             H    H                                            CH.sub.2 N(nPen)COPh                                                                     H     H    J.sup.2                                                                             H    H                                            Ph         H     H    J.sup.2                                                                             H    H                                            Bz         H     H    J.sup.2                                                                             H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     H     H    J.sup.2                                                                             H    H                                            2-thienyl  H     H    J.sup.2                                                                             H    H                                            3-furyl    H     H    J.sup.2                                                                             H    H                                            Ph(4-J.sup.2)                                                                            H     H    J.sup.2                                                                             H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      H     H    J.sup.2                                                                             H    H                                            T          H     H    J.sup.2                                                                             H    H                                            F          Cl    J.sup.1                                                                            H     H    H                                            Cl         Cl    J.sup.1                                                                            H     H    H                                            Br         Cl    J.sup.1                                                                            H     H    H                                            I          Cl    J.sup.1                                                                            H     H    H                                            Me         Cl    J.sup.1                                                                            H     H    H                                            CF.sub.3   Cl    J.sup.1                                                                            H     H    H                                            Et         Cl    J.sup.1                                                                            H     H    H                                            n-Pr       Cl    J.sup.1                                                                            H     H    H                                            c-Pr       Cl    J.sup.1                                                                            H     H    H                                            NO.sub.2   Cl    J.sup.1                                                                            H     H    H                                            NH.sub.2   Cl    J.sup.1                                                                            H     H    H                                            J.sup.1    Cl    J.sup.1                                                                            H     H    H                                            U          Cl    J.sup.1                                                                            H     H    H                                            COOMe      Cl    J.sup.1                                                                            H     H    H                                            CONH.sub.2 Cl    J.sup.1                                                                            H     H    H                                            CONHCOMe   Cl    J.sup.1                                                                            H     H    H                                            CH.sub.2 N(nPen)COPh                                                                     Cl    J.sup.1                                                                            H     H    H                                            Ph         Cl    J.sup.1                                                                            H     H    H                                            Bz         Cl    J.sup.1                                                                            H     H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     Cl    J.sup.1                                                                            H     H    H                                            2-thienyl  Cl    J.sup.1                                                                            H     H    H                                            3-furyl    Cl    J.sup.1                                                                            H     H    H                                            Ph(4-J.sup.2)                                                                            Cl    J.sup.1                                                                            H     H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Cl    J.sup.1                                                                            H     H    H                                            T          Cl    J.sup.1                                                                            H     H    H                                            F          Cl    H    J.sup.1                                                                             H    H                                            Cl         Cl    H    J.sup.1                                                                             H    H                                            Br         Cl    H    J.sup.1                                                                             H    H                                            I          Cl    H    J.sup.1                                                                             H    H                                            Me         Cl    H    J.sup.1                                                                             H    H                                            CF.sub.3   Cl    H    J.sup.1                                                                             H    H                                            Et         Cl    H    J.sup.1                                                                             H    H                                            n-Pr       Cl    H    J.sup.1                                                                             H    H                                            c-Pr       Cl    H    J.sup.1                                                                             H    H                                            NO.sub.2   Cl    H    J.sup.1                                                                             H    H                                            NH.sub.2   Cl    H    J.sup.1                                                                             H    H                                            J.sup.1    Cl    H    J.sup.1                                                                             H    H                                            U          Cl    H    J.sup.1                                                                             H    H                                            COOMe      Cl    H    J.sup.1                                                                             H    H                                            CONH.sub.2 Cl    H    J.sup.1                                                                             H    H                                            CONHCOMe   Cl    H    J.sup.1                                                                             H    H                                            CH.sub.2 N(nPen)COPh                                                                     Cl    H    J.sup.1                                                                             H    H                                            Ph         Cl    H    J.sup.1                                                                             H    H                                            Bz         Cl    H    J.sup.1                                                                             H    H                                            CH.sub.2 CH.sub.2 Ph                                                                     Cl    H    J.sup.1                                                                             H    H                                            2-thienyl  Cl    H    J.sup.1                                                                             H    H                                            3-furyl    Cl    H    J.sup.1                                                                             H    H                                            Ph(4-J.sup.2)                                                                            Cl    H    J.sup.1                                                                             H    H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Cl    H    J.sup.1                                                                             H    H                                            T          Cl    H    J.sup.1                                                                             H    H                                            F          Cl    H    H     J.sup.1                                                                            H                                            Cl         Cl    H    H     J.sup.1                                                                            H                                            Br         Cl    H    J.sup.1                                                                             H    H                                            I          Cl    H    H     J.sup.1                                                                            H                                            Me         Cl    H    H     J.sup.1                                                                            H                                            CF.sub.3   Cl    H    H     J.sup.1                                                                            H                                            Et         Cl    H    H     J.sup.1                                                                            H                                            n-Pr       Cl    H    H     J.sup.1                                                                            H                                            c-Pr       Cl    H    H     J.sup.1                                                                            H                                            NO.sub.2   Cl    H    H     J.sup.1                                                                            H                                            NH.sub.2   Cl    H    H     J.sup.1                                                                            H                                            N(Me)H     Cl    H    H     J.sup.1                                                                            H                                            N(Me).sub.2                                                                              Cl    H    H     J.sup.1                                                                            H                                            N(Me)n-Bu  Cl    H    H     J.sup.1                                                                            H                                            N(nPen)H   Cl    H    H     J.sup.1                                                                            H                                            NHCOPh     Cl    H    H     J.sup.1                                                                            H                                            N(Me)CO-c-Hex                                                                            Cl    H    H     J.sup.1                                                                            H                                            NHCONHMe   Cl    H    H     J.sup.1                                                                            H                                            N(Me)COHNPh                                                                              Cl    H    H     J.sup.1                                                                            H                                            NHCONH-c-Hex                                                                             Cl    H    H     J.sup.1                                                                            H                                            NHCOBz     Cl    H    H     J.sup.1                                                                            H                                            J.sup.1    Cl    H    H     J.sup.1                                                                            H                                            NBzCO-n-Bu Cl    H    H     J.sup.1                                                                            H                                            NBzCOO-i-Bu                                                                              Cl    H    H     J.sup.1                                                                            H                                            NHCO-n-Bu  Cl    H    H     J.sup.1                                                                            H                                            NHCOO-i-Bu Cl    H    H     J.sup.1                                                                            H                                            NHCOCF.sub.3                                                                             Cl    H    H     J.sup.1                                                                            H                                            NHSO.sub.2 CF.sub.3                                                                      Cl    H    H     J.sup.1                                                                            H                                            N(Me)Ph    Cl    H    H     J.sup.1                                                                            H                                            NHC(NH)NH.sub.2                                                                          Cl    H    H     J.sup.1                                                                            H                                            C(NH)NH.sub.2                                                                            Cl    H    H     J.sup.1                                                                            H                                            CHO        Cl    H    H     J.sup.1                                                                            H                                            CN         Cl    H    H     J.sup.1                                                                            H                                            U          Cl    H    H     J.sup.1                                                                            H                                            COOMe      Cl    H    H     J.sup.1                                                                            H                                            CONH.sub.2 Cl    H    H     J.sup.1                                                                            H                                            CONHCOMe   Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 NH.sub.2                                                                        Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 OH                                                                              Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 NHCOPh                                                                          Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 N(nPen)COPh                                                                     Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 NHCONHMe                                                                        Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 CONHPh                                                                          Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 COOH                                                                            Cl    H    H     J.sup.1                                                                            H                                            Ph         Cl    H    H     J.sup.1                                                                            H                                            Bz         Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 CH.sub.2 Ph                                                                     Cl    H    H     J.sup.1                                                                            H                                            2-thienyl  Cl    H    H     J.sup.1                                                                            H                                            3-furyl    Cl    H    H     J.sup.1                                                                            H                                            Ph(4-J.sup.2)                                                                            Cl    H    H     J.sup.1                                                                            H                                            Ph(2-Cl, 3-J.sup.1)                                                                      Cl    H    H     J.sup.1                                                                            H                                            Ph(2-Cl, 4-J.sup.1)                                                                      Cl    H    H     J.sup.1                                                                            H                                            Ph(2-Cl, 5-J.sup.1)                                                                      Cl    H    H     J.sup.1                                                                            H                                            Ph(2-Cl, 6-J.sup.1)                                                                      Cl    H    H     J.sup.1                                                                            H                                            CH.sub.2 CH.sub.2 Ph(2-Cl, 5-J.sup.1)                                                    Cl    H    H     J.sup.1                                                                            H                                            T          Cl    H    H     J.sup.1                                                                            H                                            F          Cl    H    H     H    J.sup.1                                      Cl         Cl    H    H     H    J.sup.1                                      Br         Cl    H    H     H    J.sup.1                                      I          Cl    H    H     H    J.sup.1                                      Me         Cl    H    H     H    J.sup.1                                      CF.sub.3   Cl    H    H     H    J.sup.1                                      Et         Cl    H    H     H    J.sup.1                                      N(Me)n-Bu  Cl    H    H     H    J.sup.1                                      N(nPen)H   Cl    H    H     H    J.sup.1                                      NHCOPh     Cl    H    H     H    J.sup.1                                      J.sup.1    Cl    H    H     H    J.sup.1                                      NHC(NH)NH.sub.2                                                                          Cl    H    H     H    J.sup.1                                      C(NH)NH.sub.2                                                                            Cl    H    H     H    J.sup.1                                      CHO        Cl    H    H     H    J.sup.1                                      CN         Cl    H    H     H    J.sup.1                                      U          Cl    H    H     H    J.sup.1                                      COOMe      Cl    H    H     H    J.sup.1                                      CONH.sub.2 Cl    H    H     H    J.sup.1                                      CONHCOMe   Cl    H    H     H    J.sup.1                                      CH.sub.2 N(nPen)COPh                                                                     Cl    H    H     H    J.sup.1                                      Ph         Cl    H    H     H    J.sup.1                                      Bz         Cl    H    H     H    J.sup.1                                      CH.sub.2 CH.sub.2 Ph                                                                     Cl    H    H     H    J.sup.1                                      Ph(4-J.sup.2)                                                                            Cl    H    H     H    J.sup.1                                      Ph(2-Cl, 5-J.sup.1)                                                                      Cl    H    H     H    J.sup.1                                      __________________________________________________________________________

                                      TABLE 4                                     __________________________________________________________________________     ##STR29##                                                                    R.sup.1                                                                            R.sup.3     R.sup.60                                                                          R.sup.61                                                                           R.sup.62                                                                          R.sup.63                                                                           R.sup.64                                   __________________________________________________________________________    n-Pr F           H   H    H   H    H                                          n-Pr Cl          H   H    H   H    H                                          n-Pr Br          H   H    H   H    H                                          n-Pr I           H   H    H   H    H                                          n-Pr Me          H   H    H   H    H                                          n-Pr CF.sub.3    H   H    H   H    H                                          n-Pr Et          H   H    H   H    H                                          n-Pr n-Pr        H   H    H   H    H                                          n-Pr c-Pr        H   H    H   H    H                                          n-Pr NO.sub.2    H   H    H   H    H                                          n-Pr NH.sub.2    H   H    H   H    H                                          n-Pr N(Me)n-Bu   H   H    H   H    H                                          n-Pr N(nPen)H    H   H    H   H    H                                          n-Pr NHCOPh      H   H    H   H    H                                          n-Pr U           H   H    H   H    H                                          n-Pr CONH.sub.2  H   H    H   H    H                                          n-Pr CONHCOMe    H   H    H   H    H                                          n-Pr CH.sub.2 N(nPen)COPh                                                                      H   H    H   H    H                                          n-Pr Ph(2-Cl,5-J.sup.1)                                                                        H   H    H   H    H                                          n-Pr OH          H   H    H   H    H                                          n-Pr T           H   H    H   H    H                                          Et   F           H   H    H   H    H                                          Et   Cl          H   H    H   H    H                                          Et   Br          H   H    H   H    H                                          Et   I           H   H    H   H    H                                          Et   Me          H   H    H   H    H                                          Et   CF.sub.3    H   H    H   H    H                                          Et   NO.sub.2    H   H    H   H    H                                          Et   NH.sub.2    H   H    H   H    H                                          Et   NHCOPh      H   H    H   H    H                                          Et   OH          H   H    H   H    H                                          Et   T           H   H    H   H    H                                          n-Bu F           H   H    H   H    H                                          n-Bu Cl          H   H    H   H    H                                          n-Bu Br          H   H    H   H    H                                          n-Bu I           H   H    H   H    H                                          n-Bu Me          H   H    H   H    H                                          n-Bu CF.sub.3    H   H    H   H    H                                          n-Bu NO.sub.2    H   H    H   H    H                                          n-Bu NH.sub.2    H   H    H   H    H                                          n-Bu N(Me)CO-c-Hex                                                                             H   H    H   H    H                                          n-Bu NHCONH-c-Hex                                                                              H   H    H   H    H                                          n-Bu OH          H   H    H   H    H                                          n-Bu T           H   H    H   H    H                                          n-Pr F           Me  H    H   H    H                                          n-Pr Cl          Me  H    H   H    H                                          n-Pr Br          Me  H    H   H    H                                          n-Pr I           Me  H    H   H    H                                          n-Pr Me          Me  H    H   H    H                                          n-Pr CF.sub.3    Me  H    H   H    H                                          n-Pr Et          Me  H    H   H    H                                          n-Pr n-Pr        Me  H    H   H    H                                          n-Pr c-Pr        Me  H    H   H    H                                          n-Pr NO.sub.2    Me  H    H   H    H                                          n-Pr NH.sub.2    Me  H    H   H    H                                          n-Pr NHCOPh      Me  H    H   H    H                                          n-Pr J.sup.1     Me  H    H   H    H                                          n-Pr NHC(NH)NH.sub.2                                                                           Me  H    H   H    H                                          n-Pr C(NH)NH.sub.2                                                                             Me  H    H   H    H                                          n-Pr CHO         Me  H    H   H    H                                          n-Pr CN          Me  H    H   H    H                                          n-Pr U           Me  H    H   H    H                                          n-Pr CONH.sub.2  Me  H    H   H    H                                          n-Pr CH.sub.2 N(nPen)COPh                                                                      Me  H    H   H    H                                          n-Pr Ph          Me  H    H   H    H                                          n-Pr Bz          Me  H    H   H    H                                          n-Pr CH.sub.2 CH.sub.2 Ph                                                                      Me  H    H   H    H                                          n-Pr 2-thienyl   Me  H    H   H    H                                          n-Pr 3-furyl     Me  H    H   H    H                                          n-Pr Ph(4-J.sup.2)                                                                             Me  H    H   H    H                                          n-Pr Ph(2-Cl,5-J.sup.1)                                                                        Me  H    H   H    H                                          n-Pr T           Me  H    H   H    H                                          n-Pr F           H   Me   H   H    H                                          n-Pr Cl          H   Me   H   H    H                                          n-Pr Br          H   Me   H   H    H                                          n-Pr I           H   Me   H   H    H                                          n-Pr Me          H   Me   H   H    H                                          n-Pr CF.sub.3    H   Me   H   H    H                                          n-Pr NO.sub.2    H   Me   H   H    H                                          n-Pr NH.sub.2    H   Me   H   H    H                                          n-Pr NHCOPh      H   Me   H   H    H                                          n-Pr J.sup.1     H   Me   H   H    H                                          n-Pr NHC(NH)NH.sub.2                                                                           H   Me   H   H    H                                          n-Pr C(NH)NH.sub.2                                                                             H   Me   H   H    H                                          n-Pr CHO         H   Me   H   H    H                                          n-Pr CN          H   Me   H   H    H                                          n-Pr U           H   Me   H   H    H                                          n-Pr CONH.sub.2  H   Me   H   H    H                                          n-Pr CH.sub.2 N(nPen)COPh                                                                      H   Me   H   H    H                                          n-Pr Ph          H   Me   H   H    H                                          n-Pr Bz          H   Me   H   H    H                                          n-Pr CH.sub.2 CH.sub.2 Ph                                                                      H   Me   H   H    H                                          n-Pr 2-thienyl   H   Me   H   H    H                                          n-Pr 3-furyl     H   Me   H   H    H                                          n-Pr Ph(4-J.sup.2)                                                                             H   Me   H   H    H                                          n-Pr Ph(2-Cl,5-J.sup.1)                                                                        H   Me   H   H    H                                          n-Pr T           H   Me   H   H    H                                          n-Pr F           H   H    Me  H    H                                          n-Pr Cl          H   H    Me  H    H                                          n-Pr Br          H   H    Me  H    H                                          n-Pr I           H   H    Me  H    H                                          n-Pr Me          H   H    Me  H    H                                          n-Pr CF.sub.3    H   H    Me  H    H                                          n-Pr NO.sub.2    H   H    Me  H    H                                          n-Pr NH.sub.2    H   H    Me  H    H                                          n-Pr NHCOPh      H   H    Me  H    H                                          n-Pr J.sup.1     H   H    Me  H    H                                          n-Pr NHC(NH)NH.sub.2                                                                           H   H    Me  H    H                                          n-Pr C(NH)NH.sub.2                                                                             H   H    Me  H    H                                          n-Pr CHO         H   H    Me  H    H                                          n-Pr CN          H   H    Me  H    H                                          n-Pr U           H   H    Me  H    H                                          n-Pr CONH.sub.2  H   H    Me  H    H                                          n-Pr CH.sub.2 N(nPen)COPh                                                                      H   H    Me  H    H                                          n-Pr Ph          H   H    Me  H    H                                          n-Pr Bz          H   H    Me  H    H                                          n-Pr CH.sub.2 CH.sub.2 Ph                                                                      H   H    Me  H    H                                          n-Pr 2-thienyl   H   H    Me  H    H                                          n-Pr 3-furyl     H   H    Me  H    H                                          n-Pr Ph(4-J.sup.2)                                                                             H   H    Me  H    H                                          n-Pr Ph(2-Cl,5-J.sup.1)                                                                        H   H    Me  H    H                                          n-Pr T           H   H    Me  H    H                                          n-Pr F           H   H    H   Me   H                                          n-Pr Cl          H   H    H   Me   H                                          n-Pr Br          H   H    H   Me   H                                          n-Pr I           H   H    H   Me   H                                          n-Pr Me          H   H    H   Me   H                                          n-Pr CF.sub.3    H   H    H   Me   H                                          n-Pr Et          H   H    H   Me   H                                          n-Pr n-Pr        H   H    H   Me   H                                          n-Pr c-Pr        H   H    H   Me   H                                          n-Pr NO.sub.2    H   H    H   Me   H                                          n-Pr NH.sub.2    H   H    H   Me   H                                          n-Pr NHCOPh      H   H    H   Me   H                                          n-Pr J.sup.1     H   H    H   Me   H                                          n-Pr NHC(NH)NH.sub.2                                                                           H   H    H   Me   H                                          n-Pr C(NH)NH.sub.2                                                                             H   H    H   Me   H                                          n-Pr CHO         H   H    H   Me   H                                          n-Pr CN          H   H    H   Me   H                                          n-Pr U           H   H    H   Me   H                                          n-Pr CONH.sub.2  H   H    H   Me   H                                          n-Pr CH.sub.2 N(nPen)COPh                                                                      H   H    H   Me   H                                          n-Pr Ph          H   H    H   Me   H                                          n-Pr Bz          H   H    H   Me   H                                          n-Pr CH.sub.2 CH.sub.2 Ph                                                                      H   H    H   Me   H                                          n-Pr 2-thienyl   H   H    H   Me   H                                          n-Pr 3-furyl     H   H    H   Me   H                                          n-Pr Ph(4-J.sup.2)                                                                             H   H    H   Me   H                                          n-Pr Ph(2-Cl,5-J.sup.1)                                                                        H   H    H   Me   H                                          n-Pr T           H   H    H   Me   H                                          n-Pr F           H   H    H   H    Me                                         n-Pr Cl          H   H    H   H    Me                                         n-Pr Br          H   H    H   H    Me                                         n-Pr I           H   H    H   H    Me                                         n-Pr Me          H   H    H   H    Me                                         n-Pr CF.sub.3    H   H    H   H    Me                                         n-Pr Et          H   H    H   H    Me                                         n-Pr n-Pr        H   H    H   H    Me                                         n-Pr c-Pr        H   H    H   H    Me                                         n-Pr NO.sub.2    H   H    H   H    Me                                         n-Pr NH.sub.2    H   H    H   H    Me                                         n-Pr NHCOPh      H   H    H   H    Me                                         n-Pr J.sup.1     H   H    H   H    Me                                         n-Pr NHC(NH)NH.sub.2                                                                           H   H    H   H    Me                                         n-Pr C(NH)NH.sub.2                                                                             H   H    H   H    Me                                         n-Pr CHO         H   H    H   H    Me                                         n-Pr CN          H   H    H   H    Me                                         n-Pr U           H   H    H   H    Me                                         n-Pr CONH.sub.2  H   H    H   H    Me                                         n-Pr CH.sub.2 N(nPen)COPh                                                                      H   H    H   H    Me                                         n-Pr Ph          H   H    H   H    Me                                         n-Pr Bz          H   H    H   H    Me                                         n-Pr CH.sub.2 CH.sub.2 Ph                                                                      H   H    H   H    Me                                         n-Pr 2-thienyl   H   H    H   H    Me                                         n-Pr 3-furyl     H   H    H   H    Me                                         n-Pr Ph(4-J.sup.2)                                                                             H   H    H   H    Me                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                        H   H    H   H    Me                                         n-Pr T           H   H    H   H    Me                                         n-Pr F           F   H    H   H    H                                          n-Pr Cl          F   H    H   H    H                                          n-Pr Br          F   H    H   H    H                                          n-Pr I           F   H    H   H    H                                          n-Pr Me          F   H    H   H    H                                          n-Pr CF.sub.3    F   H    H   H    H                                          n-Pr F           H   Cl   H   H    H                                          n-Pr Cl          H   Cl   H   H    H                                          n-Pr Br          H   Cl   H   H    H                                          n-Pr I           H   Cl   H   H    H                                          n-Pr Me          H   Cl   H   H    H                                          n-Pr CF.sub.3    H   Cl   H   H    H                                          n-Pr F           H   H    Br  H    H                                          n-Pr Cl          H   H    Br  H    H                                          n-Pr Br          H   H    Br  H    H                                          n-Pr I           H   H    Br  H    H                                          n-Pr Me          H   H    Br  H    H                                          n-Pr CF.sub.3    H   H    Br  H    H                                          n-Pr F           H   H    H   J.sup.2                                                                            H                                          n-Pr Cl          H   H    H   J.sup.2                                                                            H                                          n-Pr Br          H   H    H   J.sup.2                                                                            H                                          n-Pr I           H   H    H   J.sup.2                                                                            H                                          n-Pr Me          H   H    H   J.sup.2                                                                            H                                          n-Pr CF.sub.3    H   H    H   J.sup.2                                                                            H                                          n-Pr Et          H   H    H   J.sup.2                                                                            H                                          n-Pr n-Pr        H   H    H   J.sup.2                                                                            H                                          n-Pr F           Cl  H    H   H    J.sup.1                                    n-Pr Cl          Cl  H    H   H    J.sup.1                                    n-Pr Br          Cl  H    H   H    J.sup.1                                    n-Pr I           Cl  H    H   H    J.sup.1                                    n-Pr Me          Cl  H    H   H    J.sup.1                                    n-Pr CF.sub.3    Cl  H    H   H    J.sup.1                                    n-Pr Et          Cl  H    H   H    J.sup.1                                    n-Pr n-Pr        Cl  H    H   H    J.sup.1                                    __________________________________________________________________________

                                      TABLE 5                                     __________________________________________________________________________     ##STR30##                                                                    R.sup.1                                                                            R.sup.3    R.sup.60                                                                           R.sup.61                                                                           R.sup.62                                                                           R.sup.63                                                                           R.sup.64                                  __________________________________________________________________________    n-Pr F          H    H    H    H    H                                         n-Pr Cl         H    H    H    H    H                                         n-Pr Br         H    H    H    H    H                                         n-Pr I          H    H    H    H    H                                         n-Pr Me         H    H    H    H    H                                         n-Pr CF.sub.3   H    H    H    H    H                                         n-Pr Et         H    H    H    H    H                                         n-Pr n-Pr       H    H    H    H    H                                         n-Pr c-Pr       H    H    H    H    H                                         n-Pr NO.sub.2   H    H    H    H    H                                         n-Pr NH.sub.2   H    H    H    H    H                                         n-Pr N(Me)n-Bu  H    H    H    H    H                                         n-Pr N(nPen)H   H    H    H    H    H                                         n-Pr NHCOPh     H    H    H    H    H                                         n-Pr U          H    H    H    H    H                                         n-Pr CONH.sub.2 H    H    H    H    H                                         n-Pr CONHCOMe   H    H    H    H    H                                         n-Pr CH.sub.2 N(nPen)COPh                                                                     H    H    H    H    H                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                       H    H    H    H    H                                         n-Pr OH         H    H    H    H    H                                         n-Pr T          H    H    H    H    H                                         Et   F          H    H    H    H    H                                         Et   Cl         H    H    H    H    H                                         Et   Br         H    H    H    H    H                                         Et   I          H    H    H    H    H                                         Et   Me         H    H    H    H    H                                         Et   CF.sub.3   H    H    H    H    H                                         Et   NO.sub.2   H    H    H    H    H                                         Et   NH.sub.2   H    H    H    H    H                                         Et   NHCOPh     H    H    H    H    H                                         Et   OH         H    H    H    H    H                                         Et   T          H    H    H    H    H                                         n-Bu F          H    H    H    H    H                                         n-Bu Cl         H    H    H    H    H                                         n-Bu Br         H    H    H    H    H                                         n-Bu I          H    H    H    H    H                                         n-Bu Me         H    H    H    H    H                                         n-Bu CF.sub.3   H    H    H    H    H                                         n-Bu NO.sub.2   H    H    H    H    H                                         n-Bu NH.sub.2   H    H    H    H    H                                         n-Bu N(Me)CO-c-Hex                                                                            H    H    H    H    H                                         n-Bu NHCONH-c-Hex                                                                             H    H    H    H    H                                         n-Bu OH         H    H    H    H    H                                         n-Bu T          H    H    H    H    H                                         n-Pr F          Me   H    H    H    H                                         n-Pr Cl         Me   H    H    H    H                                         n-Pr Br         Me   H    H    H    H                                         n-Pr I          Me   H    H    H    H                                         n-Pr Me         Me   H    H    H    H                                         n-Pr CF.sub.3   Me   H    H    H    H                                         n-Pr Et         Me   H    H    H    H                                         n-Pr n-Pr       Me   H    H    H    H                                         n-Pr c-Pr       Me   H    H    H    H                                         n-Pr NO.sub.2   Me   H    H    H    H                                         n-Pr NH.sub.2   Me   H    H    H    H                                         n-Pr NHCOPh     Me   H    H    H    H                                         n-Pr J.sup.1    Me   H    H    H    H                                         n-Pr NHC(NH)NH.sub.2                                                                          Me   H    H    H    H                                         n-Pr C(NH)NH.sub.2                                                                            Me   H    H    H    H                                         n-Pr CHO        Me   H    H    H    H                                         n-Pr CN         Me   H    H    H    H                                         n-Pr U          Me   H    H    H    H                                         n-Pr CONH.sub.2 Me   H    H    H    H                                         n-Pr CH.sub.2 N(nPen)COPh                                                                     Me   H    H    H    H                                         n-Pr Ph         Me   H    H    H    H                                         n-Pr Bz         Me   H    H    H    H                                         n-Pr CH.sub.2 CH.sub.2 Ph                                                                     Me   H    H    H    H                                         n-Pr 2-thienyl  Me   H    H    H    H                                         n-Pr 3-furyl    Me   H    H    H    H                                         n-Pr Ph(4-J.sup.2)                                                                            Me   H    H    H    H                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                       Me   H    H    H    H                                         n-Pr T          Me   H    H    H    H                                         n-Pr F          H    Me   H    H    H                                         n-Pr Cl         H    Me   H    H    H                                         n-Pr Br         H    Me   H    H    H                                         n-Pr I          H    Me   H    H    H                                         n-Pr Me         H    Me   H    H    H                                         n-Pr CF.sub.3   H    Me   H    H    H                                         n-Pr NO.sub.2   H    Me   H    H    H                                         n-Pr NH.sub.2   H    Me   H    H    H                                         n-Pr NHCOPh     H    Me   H    H    H                                         n-Pr J.sup.1    H    Me   H    H    H                                         n-Pr NHC(NH)NH.sub.2                                                                          H    Me   H    H    H                                         n-Pr C(NH)NH.sub.2                                                                            H    Me   H    H    H                                         n-Pr CHO        H    Me   H    H    H                                         n-Pr CN         H    Me   H    H    H                                         n-Pr U          H    Me   H    H    H                                         n-Pr CONH.sub.2 H    Me   H    H    H                                         n-Pr CH.sub.2 N(nPen)COPh                                                                     H    Me   H    H    H                                         n-Pr Ph         H    Me   H    H    H                                         n-Pr Bz         H    Me   H    H    H                                         n-Pr CH.sub.2 CH.sub.2 Ph                                                                     H    Me   H    H    H                                         n-Pr 2-thienyl  H    Me   H    H    H                                         n-Pr 3-furyl    H    Me   H    H    H                                         n-Pr Ph(4-J.sup.2)                                                                            H    Me   H    H    H                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                       H    Me   H    H    H                                         n-Pr T          H    Me   H    H    H                                         n-Pr F          H    H    Me   H    H                                         n-Pr Cl         H    H    Me   H    H                                         n-Pr Br         H    H    Me   H    H                                         n-Pr I          H    H    Me   H    H                                         n-Pr Me         H    H    Me   H    H                                         n-Pr CF.sub.3   H    H    Me   H    H                                         n-Pr NO.sub.2   H    H    Me   H    H                                         n-Pr NH.sub.2   H    H    Me   H    H                                         n-Pr NHCOPh     H    H    Me   H    H                                         n-Pr J.sup.1    H    H    Me   H    H                                         n-Pr NHC(NH)NH.sub.2                                                                          H    H    Me   H    H                                         n-Pr C(NH)NH.sub.2                                                                            H    H    Me   H    H                                         n-Pr CHO        H    H    Me   H    H                                         n-Pr CN         H    H    Me   H    H                                         n-Pr U          H    H    Me   H    H                                         n-Pr CONH.sub.2 H    H    Me   H    H                                         n-Pr CH.sub.2 N(nPen)COPh                                                                     H    H    Me   H    H                                         n-Pr Ph         H    H    Me   H    H                                         n-Pr Bz         H    H    Me   H    H                                         n-Pr CH.sub.2 CH.sub.2 Ph                                                                     H    H    Me   H    H                                         n-Pr 2-thienyl  H    H    Me   H    H                                         n-Pr 3-furyl    H    H    Me   H    H                                         n-Pr Ph(4-J.sup.2)                                                                            H    H    Me   H    H                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                       H    H    Me   H    H                                         n-Pr T          H    H    Me   H    H                                         n-Pr F          H    H    H    Me   H                                         n-Pr Cl         H    H    H    Me   H                                         n-Pr Br         H    H    H    Me   H                                         n-Pr I          H    H    H    Me   H                                         n-Pr Me         H    H    Me   H    H                                         n-Pr CF.sub.3   H    H    H    Me   H                                         n-Pr Et         H    H    H    Me   H                                         n-Pr n-Pr       H    H    H    Me   H                                         n-Pr c-Pr       H    H    H    Me   H                                         n-Pr NO.sub.2   H    H    H    Me   H                                         n-Pr NH.sub.2   H    H    H    Me   H                                         n-Pr NHCOPh     H    H    H    Me   H                                         n-Pr J.sup.1    H    H    H    Me   H                                         n-Pr NHC(NH)NH.sub.2                                                                          H    H    H    Me   H                                         n-Pr C(NH)NH.sub.2                                                                            H    H    H    Me   H                                         n-Pr CHO        H    H    H    Me   H                                         n-Pr CN         H    H    H    Me   H                                         n-Pr U          H    H    H    Me   H                                         n-Pr CONH.sub.2 H    H    H    Me   H                                         n-Pr CH.sub.2 N(nPen)COPh                                                                     H    H    H    Me   H                                         n-Pr Ph         H    H    H    Me   H                                         n-Pr Bz         H    H    H    Me   H                                         n-Pr CH.sub.2 CH.sub.2 Ph                                                                     H    H    H    Me   H                                         n-Pr 2-thienyl  H    H    H    Me   H                                         n-Pr 3-furyl    H    H    H    Me   H                                         n-Pr Ph(4-J.sup.2)                                                                            H    H    H    Me   H                                         n-Pr Ph(2-Cl,5-J.sup.1)                                                                       H    H    H    Me   H                                         n-Pr T          H    H    H    Me   H                                         n-Pr F          H    H    H    H    Me                                        n-Pr Cl         H    H    H    H    Me                                        n-Pr Br         H    H    H    H    Me                                        n-Pr I          H    H    H    H    Me                                        n-Pr Me         H    H    H    Me   H                                         n-Pr CF.sub.3   H    H    H    H    Me                                        n-Pr Et         H    H    H    H    Me                                        n-Pr n-Pr       H    H    H    H    Me                                        n-Pr c-Pr       H    H    H    H    Me                                        n-Pr NO.sub.2   H    H    H    H    Me                                        n-Pr NH.sub.2   H    H    H    H    Me                                        n-Pr NHCOPh     H    H    H    H    Me                                        n-Pr J.sup.1    H    H    H    H    Me                                        n-Pr NHC(NH)NH.sub.2                                                                          H    H    H    H    Me                                        n-Pr C(NH)NH.sub.2                                                                            H    H    H    H    Me                                        n-Pr CHO        H    H    H    H    Me                                        n-Pr CN         H    H    H    H    Me                                        n-Pr U          H    H    H    H    Me                                        n-Pr CONH.sub.2 H    H    H    H    Me                                        n-Pr CH.sub.2 N(nPen)COPh                                                                     H    H    H    H    Me                                        n-Pr Ph         H    H    H    H    Me                                        n-Pr Bz         H    H    H    H    Me                                        n-Pr CH.sub.2 CH.sub.2 Ph                                                                     H    H    H    H    Me                                        n-Pr 2-thienyl  H    H    H    H    Me                                        n-Pr 3-furyl    H    H    H    H    Me                                        n-Pr Ph(4-J.sup.2)                                                                            H    H    H    H    Me                                        n-Pr Ph(2-Cl,5-J.sup.1)                                                                       H    H    H    H    Me                                        n-Pr T          H    H    H    H    Me                                        n-Pr F          F    H    H    H    H                                         n-Pr Cl         F    H    H    H    H                                         n-Pr Br         F    H    H    H    H                                         n-Pr I          F    H    H    H    H                                         n-Pr Me         F    H    H    H    H                                         n-Pr CF.sub.3   F    H    H    H    H                                         n-Pr F          H    Cl   H    H    H                                         n-Pr Cl         H    Cl   H    H    H                                         n-Pr Br         H    Cl   H    H    H                                         n-Pr I          H    Cl   H    H    H                                         n-Pr Me         H    Cl   H    H    H                                         n-Pr CF.sub.3   H    Cl   H    H    H                                         n-Pr F          H    H    Br   H    H                                         n-Pr Cl         H    H    Br   H    H                                         n-Pr Br         H    H    Br   H    H                                         n-Pr I          H    H    Br   H    H                                         n-Pr Me         H    H    Br   H    H                                         n-Pr CF.sub.3   H    H    Br   H    H                                         n-Pr F          H    H    H    J.sup.2                                                                            H                                         n-Pr Cl         H    H    H    J.sup.2                                                                            H                                         n-Pr Br         H    H    H    J.sup.2                                                                            H                                         n-Pr I          H    H    H    J.sup.2                                                                            H                                         n-Pr Me         H    H    H    J.sup.2                                                                            H                                         n-Pr CF.sub.3   H    H    H    J.sup.2                                                                            H                                         n-Pr Et         H    H    H    J.sup.2                                                                            H                                         n-Pr n-Pr       H    H    H    J.sup.2                                                                            H                                         n-Pr F          Cl   H    H    H    J.sup.1                                   n-Pr Cl         Cl   H    H    H    J.sup.1                                   n-Pr Br         Cl   H    H    H    J.sup.1                                   n-Pr I          Cl   H    H    H    J.sup.1                                   n-Pr Me         Cl   H    H    H    J.sup.1                                   n-Pr CF.sub.3   Cl   H    H    H    J.sup.1                                   n-Pr Et         Cl   H    H    H    J.sup.1                                   n-Pr n-Pr       Cl   H    H    H    J.sup.1                                   __________________________________________________________________________

REFERENTIAL EXAMPLE 1 (2-Phenylethyl)-3-amino-4-ethoxycarbonylpyrazole

Method A:

Step 1-A-1:

Benzaldehyde (2-phenylethyl)hydrazone

100 ml of aqueous 10% sodium hydroxide solution were added to an aqueoussolution (50 ml) of 14.55 g of (2-phenylethyl)hydrazine sulfate, and2.25 g of sodium hydroxide were added thereto and stirred at roomtemperature for one hour. The reaction solution was extracted with 250ml of dichloromethane, dried over magnesium sulfate, concentrated underreduced pressure and dried. The resulting residue was dissolved in 100ml of ethanol, and 5.55 g of benzaldehyde were added thereto and heatedunder reflux for 6 hours. This reaction solution was concentrated underreduced pressure and dried to obtain 11.38 g of a crude product of theintended compound as an yellow oil.

Step 1-A-2:

Ethyl 3- benzylidene(2-phenylethyl)hydrazino!-2-cyanoacrylate

6.19 g of ethyl ethoxymethylenecyanoacetate were added to a toluenesolution of 11.38 g of benzaldehyde(2-phenylethyl)-hydrazone and heatedunder reflux for 9 hours, and the solvent was distilled off underreduced pressure. The resulting residue was subjected to silica gelcolumn chromatography (n-hexane--ethyl acetate=4:1→ethyl acetate) andthen recrystallized from n-hexane--ethyl acetate to obtain 8.94 g of theintended compound as pale yellow crystals. m.p.: 128.9° to 132.9° C.

Step 1-A-3:

1-(2-Phenylethyl)-3-amino-4-ethoxycarbonylpyrazole

30 ml of ethanol and 4.6 ml of concentrated hydrochloric acid were addedto 8.89 g of ethyl 3-benzylidene(2-phenylethyl)hydrazino!-2-cyanoacrylate and heated underreflux for one hour. After cooled, the solvent was distilled off underreduced pressure. The resulting residue was dissolved in dichloromethaneand washed with 20 ml of aqueous 10% sodium hydroxide solution. Theaqueous phase was extracted with 100 ml of dichloromethane. Thethus-obtained organic phases were combined, dried over magnesium sulfateand then concentrated under reduced pressure. The resulting residue wassubjected to silica gel column chromatography (n-hexane--ethylacetate=3:1→2:1→1:1) to obtain 5.61 g of the intended compound ascolorless crystals. m.p.: 76.9° to 78.6° C.

Method B:

250 ml of toluene and 0.1 ml of aqueous 12.5 M sodium hydroxide solutionwere added to a mixture of 15.69 g of ethyl3-amino-4-pyrazolecarboxylate, 24.34 g of (2-bromoethyl)benzene, 2.54 gof Adogen 464 and 27.74 g of potassium carbonate, and heated underreflux for 2.5 hours. The reaction solution was washed with 200 ml ofwater and dried over magnesium sulfate, and the solvent was distilledoff under reduced pressure. The resulting residue was subjected tosilica gel column chromatography (n-hexane--ethyl acetate=2:1→1:1→1:2)to obtain 16.94 g of 1-(2-phenylethyl)-3-amino-4-ethoxycarbonylpyrazoleas colorless crystals.

REFERENTIAL EXAMPLE 2

N- 1-(2-phenylethyl)-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!amine

2.1 ml of 1.5M lithium diisopropylamide/cyclohexane solution were addedto THF solution (35 ml) containing 363 mg of1-(2-phenylethyl)-3-amino-4-ethoxycarbonylpyrazole and 0.40 ml of1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone, while cooling withdry ice-acetone, and stirred at room temperature for 15 minutes. Themixture was again cooled with dry ice-acetone, and 10 ml of THF solutionof 877 mg of 4-bromomethyl-2'-N-triphenylmethyl-(1H-tetrazol-5-yl)!biphenyl were added thereto andstirred at room temperature for 5.5 hours. 10 ml of aqueous ammoniumchloride solution was added to the reaction solution, THF was distilledoff under reduced pressure, and the resultant was extracted with 50 mlof dichloromethane. The resulting extract was dried over magnesiumsulfate and concentrated under reduced pressure. The residue thusobtained was subjected to silica gel column chromatography(n-hexane--ethyl acetate=3:1→2:1) to obtain 234 mg of the intendedcompound as a pale yellow, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ1.22(t, J=7 Hz, 6H),

3.18 (t, J=7 Hz, 2H), 3.8-4.1 (m, 6H),

5.62 (t, J=6 Hz, 1H), 6.3-8.0 (m, 28H)

REFERENTIAL EXAMPLE 3

N- 1-(2-phenylethyl)-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamine

0.60 ml of 1.5M lithium diisopropylamide/cyclohexane solution were addedto THF solution (20 ml) containing 223 mg of N-1-(2-phenylethyl)-4-ethoxycarbonylpyrazol-3-yl)-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!amine and0.18 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone andstirred for 15 minutes, while cooling with dry ice-acetone. 0.15 ml of1-iodopropane were added to the reaction solution and stirred overnightat room temperature. 10 ml of aqueous ammonia chloride solution wereadded thereto, THF was distilled off under reduced pressure, and theresultant was extracted with 50 ml of dichloromethane. The resultingextract was dried over magnesium sulfate and concentrated under reducedpressure. The thus-obtained residue was subjected to silica gel columnchromatography (n-hexane--ethyl acetate=4:1→3:1) to obtain 91 mg of theintended compound as a pale yellow, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.81 (t, J=7 Hz, 3H),

1.1-1.8 (m, 2H),

1.22 (t, J=7 Hz, 3H),

2.8-3.3 (m, 4H),

3.99 (t, J=7 Hz, 3H),

4.15 (q, J=7 Hz, 2H),

4.45 (s, 2H), 6.7-7.9 (m, 28H)

Best Mode for Carrying Out the Invention

SYNTHESIS EXAMPLE 1

N-(1-(2-phenylethyl)-4-ethoxycarbonyl-5-bromopyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))-biphenyl-4-yl)methyl!-n-propylamine

1.52 ml of 1.0M lithium bis(trimethylsilyl)amide/hexane solution wereadded to THF solution (20 ml) containing 395 mg of N-1-(2-phenylethyl)-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamineand 0.18 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone, atroom temperature, and then heated under reflux for 30 minutes. 0.60 mlof 1,2-dibromo-1,1,2,2-tetrafluoroethane was added thereto and heatedunder reflux for further 30 minutes. 10 ml of ammonium chloride wereadded to the reaction solution, THF was distilled off under reducedpressure, and the resultant was extracted with 150 ml ofdichloromethane. The resulting extract was dried over magnesium sulfateand subjected to silica gel column chromatography (n-hexane--ethylacetate=2:1) to obtain 363 mg of the intended compound as a pale red,amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.81(t, J=7 Hz, 3H),

1.2-1.8(m, 2H), 1.28(t, J=7 Hz, 3H),

2.8-3.2(m, 4H), 4.0-4.5(m, 4H),

4.32(s, 2H), 6.7-7.5(m, 27H),

7.7-7.9(m, 1H)

MS(FAB): 857(M+H)

SYNTHESIS EXAMPLE 2

N- 1-(2-phenylethyl)-4-ethoxycarbonyl-5-bromopyrazol-3-yl!-N-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl!-n-propylamine

356 mg of N- 1-(2-phenylethyl)-4-ethoxycarbonyl-5-bromopyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylaminewere dissolved in 5 ml of ethanol and heated under reflux for 2 hours,and the solvent was distilled off under reduced pressure. The resultingresidue was subjected to silica gel column chromatography(n-hexane--ethyl acetate=2:1→ethyl acetate) to obtain 224 mg of theintended compound as a pale yellow, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.87(t, J=7 Hz, 3H),

1.1-1.7(m, 2H), 2.8-3.4(m, 4H),

4.31(s, 2H), 4.0-4.5(m, 4H),

6.8-7.5(m, 12H), 7.7-7.9(m, 1H)

SYNTHESIS EXAMPLE 3

N- 1-(2-phenylethyl)-4-carboxy-5-bromopyrazol-3-yl!-N-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl!-n-propylamine

5 ml of ethanol, 5 ml of water and 226 mg of potassium hydroxide wereadded to 206 mg of N-1-(2-phenylethyl)-4-ethoxycarbonyl-5-bromopyrazol-3-yl!-N-(2'-(1H-tetrazol-5-yl)-biphenyl-4-yl)methyl!-n-propylamine, and heatedunder reflux for 5 hours. Ethanol was distilled off under reducedpressure, and 10 ml of water were added to the reaction mixture, whichwas then made acidic with concentrated hydrochloric acid. The resultantwas extracted with 50 ml of dichloromethane. After dried over magnesiumsulfate, the extract was concentrated under reduced pressure and driedto obtain 185 mg of the intended compound as a pale yellow, amorphoussolid.

¹ H NMR(CDCl₃, 60 MHz): δ0.91(t, J=7 Hz, 3H),

1.1-1.8(m, 2H), 3.09(t, J=7 Hz, 4H),

4.07(s, 2H), 4.38(t, J=7 Hz, 2H),

6.90(s, 5H), 7.0-7.5(m, 12H),

7.7-7.9(m, 1H), 10.8-11.5(m, 2H)

MS(FAB): 586(M+H)

SYNTHESIS EXAMPLE 4

N- 1-(2-phenylethyl)-4-carboxy-5-bromopyrazol-3-yl!-N-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl!-n-propylamine dipotassiumsalt

102 mg of N- 1-(2-phenylethyl)-4-carboxy-5-bromopyrazol-3-yl!-N-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl!-n-propylamine were dissolvedin 2 ml of methanol, and 3.5 ml of 0.1M potassium hydroxide/methanolsolution were added thereto and stirred at room temperature for onehour. The resultant was concentrated under reduced pressure and dried toobtain 107 mg of the intended compound as an yellow, amorphous solid.

MS(FAB) : 662(M+H)

SYNTHESIS EXAMPLE 5

N- 1-(2-phenylethyl)-5-iodo-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))-biphenyl-4-yl)methyl!-n-propylamine

0.18 ml of 1.6M n-butyl lithium/hexane solution were added to THFsolution (10 ml) of 202 mg of N-1-(2-phenylethyl)-5-bromo-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamine,while cooling with dry ice-acetone. After stirred for 2 hours, 667 mg of1,2-diiodoethane were added thereto. After stirred for one hour, themixture was then stirred at room temperature for further one hour. 10 mlof aqueous ammonium chloride solution were added to the reactionsolution, THF was distilled off under reduced pressure, and theresultant was extracted with 50 ml of dichloromethane. After dried overmagnesium sulfate, this was subjected to silica gel columnchromatography (n-hexane--ethyl acetate=5:1) to obtain 84 mg of theintended compound as a pale red, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.77(t, J=7 Hz, 3H),

1.31(t, J=7 Hz, 3H), 1.3-1.8(m, 2H),

2.8-3.2(m, 4H), 4.22(q, J=7 Hz, 2H),

4.28(t, J=7 Hz, 2H), 4.31(s, 2H),

6.8-7.5(m, 27H), 7.6-7.9(m, 1H)

MS(FAB): 904(M+H)

SYNTHESIS EXAMPLE 6

N- 1-(2-phenylethyl)-5-chloro-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))-biphenyl-4-yl)methyl!-n-propylamine

0.24 ml of 1.6M n-butyl lithium/hexane solution were added to THFsolution (10 ml) of 231 mg of N-1-(2-phenylethyl)-5-bromo-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamine,while cooling with dry ice-acetone. After stirred for 30 minutes, 49 mgof N-chlorosuccinimide were added thereto and stirred for 30 minutes. 10ml of aqueous ammonium chloride solution were added to the reactionsolution, THF was distilled off under reduced pressure, and theresultant was extracted with 50 ml of dichloromethane. After dried overmagnesium sulfate, the resultant was subjected to silica gel columnchromatography (n-hexane--ethyl acetate=5:1) to obtain 159 mg of theintended compound as a pale yellow, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.78(t, J=7 Hz, 3H),

1.27(t, J=7 Hz, 3H), 1.3-1.8(m, 2H),

2.99(t, J=7 Hz, 4H),

3.12(t, J=7 Hz, 4H),

4.23(q, J=7 Hz, 2H),

4.29(t, J=7 Hz, 2H), 4.36(s, 2H),

6.7-7.6(m, 27H), 7.8-8.0(m, 1H)

MS(FAB): 812(M+H)

SYNTHESIS EXAMPLE 7

N- 1-(2-phenylethyl)-5-(n-butylamino)-4-ethoxycarbonyl-pyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamine

30 mg of reduced copper, 20 mg of copper(II) oxide, 83 mg of potassiumcarbonate and 5 ml of n-butylamine were added to 216 mg of N-1-(2-phenylethyl)-5-bromo-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamine,and heated under reflux for 14 hours. The reaction solution was filteredthrough Celite, and the filtrate was concentrated under reducedpressure. The residue was subjected to silica gel column chromatography(n-hexane--ethyl acetate=7:1) to obtain 92 mg of the intended compoundas a pale yellow, amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.75(t, J=7 Hz, 3H),

0.89(t, J=7 Hz, 3H),

1.21(t, J=7 Hz, 3H), 1.1-1.8(m, 6H),

2.99(t, J=7 Hz, 6H),

4.04(t, J=7 Hz, 2H),

4.17(q, J=7 Hz, 2H),

4.31(s, 2H), 5.91(t, J=7 Hz, 1H),

6.7-7.5(m, 27H), 7.6-7.9(m, 1H)

SYNTHESIS EXAMPLE 8

N-1-(2-phenylethyl)-5-(2-methylphenyl)-4-ethoxy-carbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamin

0.23 ml of 1.6M n-butyl lithium/hexane solution were dropwise added toTHF solution (5 ml) containing 208 mg of N-1-(2-phenylethyl)-5-bromo-4-ethoxycarbonylpyrazol-3-yl!-N-(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl))biphenyl-4-yl)methyl!-n-propylamineand 0.04 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone andstirred for 10 minutes, while cooling with dry ice-acetone. 0.74 ml of0.5M zinc chloride/THF solution were added thereto and stirred for 30minutes at room temperature. Then, THF solution (5 ml) containing 83 mgof m-iodotoluene and 36 mg of tetrakis(triphenylphosphine) palladium(0)were added thereto and stirred for 28 hours at 60° C. 10 ml of ammoniumchloride were added to the reaction solution, THF was distilled offunder reduced pressure, and the resultant was extracted with 50 ml ofdichloromethane. After dried over magnesium sulfate, the solvent wasdistilled off under reduced pressure. The resulting residue wassubjected to silica gel column chromatography (n-hexane--ethylacetate=5:1) to obtain 171 mg of the intended compound as a pale yellow,amorphous solid.

¹ H NMR(CDCl₃, 60 MHz): δ0.82(t, J=7 Hz, 6H), 1.3-1.8(m, 2H),

2.22(s, 3H), 2.96(t, J=7 Hz, 2H),

3.20(t, J=7 Hz, 2H), 3.7-4.1(m, 4H),

4.44(s, 2H), 6.3-7.5(m, 31H),

7.7-7.9(m, 1H)

MS(FAB): 868(M+H)

SYNTHESIS EXAMPLES 9 TO 21

In the same manner as in Synthesis Example 8, the following compoundswere synthesized.

    __________________________________________________________________________     ##STR31##                                                                    No.*                                                                             R.sup.3    .sup.1 H NMR, MS                                                __________________________________________________________________________     9                                                                                ##STR32## MS(FAB): 868(M+H)                                               10                                                                                ##STR33## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.82(t, J=7Hz,                       3H), 0.85(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.22(s, 3H),                        2.95(t, J=7Hz, 2H), 3.18(t, J=7Hz, 2H), 3.87 (t, J=7Hz,                       2H), 3.90(q, J=7Hz, 2H), 4.42(s, 2H), 6.5-7.4(m, 31H),                        7.6-7.9 (m, 1H) MS(FAB): 868(M+H)                               11                                                                                ##STR34## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 0.84(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.97(t, J=7Hz,                      2H), 3.87(t, J=7Hz, 2H), 3.88(q, J=7Hz, 2H), 4.45(s, 2H),                     6.5-7.5(m, 32H), 7.7-8.0(m, 1H) MS(FAB): 854(M+H)               12                                                                                ##STR35## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.81(t, J=7H, 6H),                   1.2-1.8(m, 2H), 2.7- 3.4(m, 4H), 366(s, 3H), 3.89(q, J=7Hz,                   2H), 3.90(t, J=7Hz, 2H), 4.46(s, 2H), 6.4-7.5(m, 31H),                        7.6-7.9(m, 1H) MS(FAB): 884(M+H)                                13                                                                                ##STR36## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.83(t, J=7Hz,                       6H), 1.3-1.9(m, 2H), 2.97 (t, J=7Hz, 2H), 3.21(t, J=7Hz,                      2H), 3.67(s, 3H), 3.90(q, J=7Hz, 2H), 3.90 (t, J=7Hz, 2H),                    4.45(s, 2H), 6.2-7.5(m, 31H), 7.6-7.9(m, 1H) MS(FAB):                         884(M+H)                                                        14                                                                                ##STR37## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.72(t, J=7Hz,                       3H), 0.88(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.95(t, J=7Hz,                      2H), 3.21(t, J=7Hz, 2H), 3.78(s, 3H), 3.88 (t, J=7Hz, 2H),                    3.93(q, J=7Hz, 2H), 4.44(s, 2H), 6.6-7.5(m, 31H), 7.6-8.0                     (m, 1H) MS(FAB): 884(M+H)                                       15                                                                                ##STR38## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.77(t, J=7Hz,                       3H), 0.82(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.8-3.4(m, 4H),                     3.87(q, J=7Hz, 2H), 4.06(t, J=7Hz, 2H), 4.46(s, 2H),                          6.1-8.0(m, 32H)                                                 16                                                                                ##STR39## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 0.81(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.94(t, J=7Hz,                      2H), 3.20(t, J=7Hz, 2H), 3.83(t, J=7Hz, 2H), 3.87(q, J=7Hz,                   2H), 4.43(s, 2H), 6.4-7.5(m, 31H), 7.6-7.9(m, 1H)               17                                                                                ##STR40## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 0.90(t, J=7Hz, 3H), 1.3- 1.8(m, 2H), 2.8-3.4(m, 4H),                     3.93(q, J=7Hz, 2H), 4.02(t, J=7Hz, 2H), 4.39(s, 2H),                          6.4-7.5(m, 30H), 7.7-7.9(m, 1H) MS(FAB): 933(M+H)               18                                                                                ##STR41## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.81(t, J=7Hz,                       3H), 0.92(t, J=7Hz, 3H), 1.3- 1.8(m, 2H), 2.99(t, J=7Hz,                      2H), 3.19(t, J=7Hz, 2H), 3.98(q, J=7Hz, 2H), 3.99(t, J=7Hz,                   2H), 4.46(s, 2H), 6.3-7.5(m, 30H), 7.6-8.0(m, 1H) MS(FAB):                    869(M+H)                                                        19                                                                                ##STR42## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 1.15(t, J=7Hz, 3H), 1.3- 1.8(m, 2H), 2.82(t, J=7Hz,                      2H), 3.12(t, J=7Hz, 2H), 3.95(s, 2H), 3.95 (t, J=7Hz, 2H),                    4.15(q, J=7Hz, 2H), 4.38(s, 2H), 6.6-7.4(m, 32H), 7.5-7.9                     (m, 1H)                                                         20                                                                                ##STR43## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.77(t, J=7Hz,                       3H), 2.24(t, J=7Hz, 3H), 1.2- 1.8(m, 2H), 2.98(t, J=7Hz,                      2H), 3.10(t, J=7Hz, 2H), 3.34(d, J=6Hz, 2H), 4.02(t, J=7Hz,                   2H), 4.18(q, J=7Hz, 2H), 4.34(s, 2H), 4.6-5.1(m, 2H),                         5.3-5.8(m, 1H), 6.8-7.5(m, 27H), 7.6-7.9(m, 1H) MS(FAB):                      818(M+H)                                                        21                                                                                ##STR44## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.67(t, J=7Hz,                       3H), 0.80(t, J=7Hz, 3H), 1.1- 1.8(m, 2H), 3.10(t, J=7Hz,                      2H), 3.69(q, J=7Hz, 2H), 4.10(t, J=7Hz, 4H), 4.50(s, 2H),                     6.8-7.5(m, 33H) MS(FAB): 882(M+H)                               __________________________________________________________________________     *Synthesis Example No.                                                   

SYNTHESIS EXAMPLES 22 TO 37

The he following compounds were synthesized by deprotecting thecorresponding compounds in the same manner as in Synthesis Example 2.

    __________________________________________________________________________     ##STR45##                                                                    No.*                                                                             R.sup.3    .sup.1 H NMR, MS                                                __________________________________________________________________________    22 Cl         .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.82(t, J=7Hz,                       3H), 1.27(t, J=7Hz, 3H), 1.3-                                                 1.8(m, 2H), 2.99(t, J=7Hz, 2H), 3.12(t, J=7Hz, 2H), 4.18(t,                   J=7Hz, 2H),                                                                   4.19(q, J=7Hz, 2H), 4.36(s, 2H), 6.7-7.6(m, 12H),                             7.8-8.1(m, 1H)                                                                MS(EI): 288(9%), 334(17%), 526(7%), 596(M.sup.+, 1%)            23 I          .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.83(t, J=7Hz,                       3H), 1.32(t, J=7Hz, 3H), 1.3-                                                 1.8(m, 2H), 2.98(t, J=7Hz, 2H), 3.12(t, J=7Hz, 2H), 4.21(q,                   J=7Hz, 2H),                                                                   4.28(t, J=7Hz, 2H), 4.37(s, 2H), 6.7-7.6(m, 12H),                             7.8-8.0(m, 1H)                                                                MS(EI): 380(48%), 426(66%), 618(77%), 661(M.sup.+, 8%)          24                                                                                ##STR46## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.71(t, J=7Hz,                       3H), 0.89(t, J=7Hz, 3H), 1.3- 1.8(m, 2H), 1.91(s, 3H),                        2.93(t, J=7Hz, 2H), 3.25(t, J=7Hz, 2H), 3.77 (t, J=7Hz,                       2H), 3.95(q, J=7Hz, 2H), 4.51(s, 2H), 6.75(d, J=8Hz, 12H),                    7.20 (s, 9H), 7.49(d, J=8Hz, 4H) MS(ET): 344(16%),                            391(37%), 508(4%), 625(M.sup.+, 0.4%)                           25                                                                                ##STR47## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.77(t, J=7Hz,                       3H), 0.88(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.24(s, 3H),                        2.94(t, J=7Hz, 2H), 3.24(t, J=7Hz, 2H), 3.83 (q, J=7Hz,                       2H), 3.86(t, J=7Hz, 2H), 4.45(s, 2H), 6.3-7.5(m, 16H),                        7.7-8.0 (m, 1H), 9.2-9.7(m, 1H) MS(FAB): 626(M+H)               26                                                                                ##STR48## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 0.85(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.30(s, 3H),                        2.89(t, J=7Hz, 2H), 3.17(t, J=7Hz, 2H), 3.83 (q, J=7Hz,                       2H), 3.86(t, J=7Hz, 2H), 4.41(s, 2H), 6.4-7.6(m, 16H),                        7.8-8.0 (m, 1H) MS(EI): 344(4%), 391(5%), 582(3%),                            625(M.sup.+, 1%)                                                27                                                                                ##STR49## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.76(t, J=7Hz,                       3H), 0.88(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.91(t, J=7Hz,                      2H), 3.22(t, J=7Hz, 2H), 3.82(q, J=7Hz, 2H), 3.87(t, J=7Hz,                   2H), 4.47(s, 2H), 6.5-7.6(m, 17H), 7.8-8.1(m, 1H)               28                                                                                ##STR50## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.75(t, J=7Hz,                       3H), 0.84(t, J=7Hz, 3H), 1.2- 1.8(m, 2H), 2.7-3.3(m, 4H),                     3.65(s, 3H), 3.82(q, J=7Hz, 2H), 4.04(t, J=7Hz, 2H),                          4.42(s, 2H), 6.4-7.6(m, 17H), 7.8-8.1(m, 1H) MS(EI):                          360(24%), 407(100%), 598(4%), 642(M.sup.+ +H, 3%)               29                                                                                ##STR51## MS(EI): 361(7%), 407(24%), 598(2%), 641(M.sup.+, 1%)            30                                                                                ##STR52## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.86(t, J=7Hz,                       3H), 0.88(t, J=7Hz, 3H), 1.2- 1.8(m, 2H), 2.91(t, J=7Hz,                      2H), 3.22(t, J=7Hz, 2H), 3.27(s, 3H), 3.86 (q, J=7Hz, 2H),                    3.88(t, J=7Hz, 2H), 4.46(s, 2H), 6.4-7.5(m, 16H), 7.8-8.0                     (m, 1H) MS(EI): 360(3%), 407(10%), 598(0.7%), 641(M.sup.+,                    0.5%)                                                           31                                                                                ##STR53## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.74(t, J=7Hz,                       3H), 0.87(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.99(t, J=7Hz,                      2H), 3.25(t, J=7Hz, 2H), 3.83(q, J=7Hz, 2H), 4.06(t, J=7Hz,                   2H), 4.49(s, 2H), 6.2-7.6(m, 16H), 7.8-8.1(m, 1H)               32                                                                                ##STR54## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.79(t, J=7Hz,                       3H), 0.91(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.93(t, J=7Hz,                      2H), 3.25(t, J=7Hz, 2H), 3.84(q, J=7Hz, 2H), 3.87(t, J=7Hz,                   2H), 4.48(s, 2H), 6.4-6.7(m, 4H), 6.8-7.5(m, 12H), 7.7-                       8.0(m, 1H) MS(FAB): 646(M+H)                                    33                                                                                ##STR55## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.89(t, J=7Hz,                       6H), 1.3-1.9(m, 2H), 2.98 (t, J=7Hz, 2H), 3.22(t, J=7Hz,                      2H), 3.89(q, J=7Hz, 2H), 4.00(t, J=7Hz, 2H), 4.45(s, 2H),                     6.4-7.6(m, 15H), 7.8-8.1(m, 1H) MS(EI): 411(5%), 456(10%),                    647(1%), 690(M.sup.+, 0.2%)                                     34                                                                                ##STR56## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.87(t, J=7Hz,                       3H), 0.90(t, J=7Hz, 3H), 1.3- 1.9(m, 2H), 2.97(t, J=7Hz,                      2H), 3.21(t, J=7Hz, 2H), 3.91(q, J=7Hz, 2H), 3.97(t, J=7Hz,                   2H), 4.47(s, 2H), 6.3-7.6(m, 15H), 7.8-8.1(m, 1H), 8.3-                       8.8(m, 1H) MS(EI): 336(34%), 383(37%), 531(14%), 574(14%),                    617(M.sup.+, 0.8%)                                              35                                                                                ##STR57## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.83(t, J=7Hz,                       3H), 1.13(t, J=7Hz, 3H), 1.3- 1.8(m, 2H), 2.78(t, J=7Hz,                      2H), 3.14(t, J=7Hz, 2H), 3.95(s, 2H), 3.95 (t, J=7Hz, 2H),                    4.11(q, J=7Hz, 2H), 4.36(s, 2H), 6.7-7.6(m, 17H), 7.8-8.1                     (m, 1H), 9.9-10.6(m, 1H) MS(EI): 316(8%), 344(13%),                           390(12%), 582(5%), 625(M.sup.+, 3%)                             36                                                                                ##STR58## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.72(t, J=7Hz,                       3H), 1.24(t, J=7Hz, 3H), 1.2- 1.8(m, 2H), 2.8-3.5(m, 6H),                     4.01(t, J=7Hz, 2H), 4.17(q, J=7Hz, 2H), 4.35(s, 2H),                          4.6-5.1(m, 2), 5.3-5.9(m, 1H), 6.8-7.6(m, 12H), 7.8-8.1(m,                    1H), 9.1-9.6(m, 1H)                                             37                                                                                ##STR59## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.65(t, J=7Hz,                       3H), 0.89(J=7Hz, 3H), 1.3- 1.9(m, 2H), 3.12(t, J=7Hz, 2H),                    3.65(q, J=7Hz, 2H), 4.09(t, J=7Hz, 4H), 4.51(s, 2H),                          6.8-7.5(m, 18H), 7.8-8.1(m, 1H) MS(FAB): 640(M+H)               38 NH.sup.n Pr                                                                              .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.6-1.1(m, 6H),                      1.2-1.8(m, 6H), 1.26(t, J=                                                    7Hz, 3H), 2.7-3.2(m, 6H), 3.97(t, J=7Hz, 2H), 4.16(q,                         J=7Hz, 4H), 4.23                                                              (s, 2H), 6.7-7.5(m, 12H), 7.7-8.0(m, 1H)                                      MS(EI): 325(5%), 372(2%), 517(4%), 563(0.8%), 606(M.sup.+,                    1%)                                                             __________________________________________________________________________     *Synthesis Example No.                                                   

SYNTHESIS EXAMPLES 39 TO 55

The following compounds were synthesized by hydrolyzing thecorresponding esters in the same manner as in Synthesis Example 3.

    __________________________________________________________________________     ##STR60##                                                                    No.*                                                                             R.sup.3    .sup.1 H NMR, MS                                                __________________________________________________________________________    39 Cl         .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.88(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 3.08                                                     (t, J=7Hz, 4H), 4.08(s, 2H), 4.33(t, J=7Hz, 2H), 6.9-7.6(m,                   12H), 7.7-8.0                                                                 (m, 1H), 9.4-10.3(m, 2H)                                                      MS(EI): 426(0.9%), 454(0.8%), 468(1%), 497(M.sup.+ -CO.sub.2                  , 2%)                                                           40 I          .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.80(t, J=7Hz,                       3H), 1.3-1.7(m, 2H), 3.13                                                     (t, J=7Hz, 4H), 4.10(s, 2H), 4.45(t, J=7Hz, 2H), 6.9-7.6(m,                   12H), 7.7-8.1                                                                 (m, 1H), 9.5-10.2(m, 2H)                                                      MS(FAB): 598(M+H)                                               41                                                                                ##STR61## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.98(t, J=7Hz,                       3H), 1.3-2.0(m, 2H), 1.75 (s, 3H), 2.9-3.5(m, 4H), 3.94(t,                    J=7Hz, 2H), 4.18(s, 2H), 6.4-7.6(m, 16H), 7.8-8.0(m, 1H),                     9.4-10.1(m, 2H) MS(EI): 105(100%), 318(2%), 509(2%),                          553(M.sup.+ -CO.sub.2, 7%)                                      42                                                                                ##STR62## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.95(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 2.19 (s, 3H), 2.05(t, J=7Hz, 2H),                        2.16(t, J=7Hz, 2H), 4.15(t, J=7Hz, 2H), 4.17 (s, 2H),                         6.4-7.6(m, 16H), 7.7-8.0(m, 1H), 11.4-12.1(m, 2H)               43                                                                                ##STR63## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.94(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 2.31 (s, 3H), 3.04(t, J=7Hz, 2H),                        3.25(t, J=7Hz, 2H), 4.15(t, J=7Hz, 2H), 4.20 (s, 2H),                         6.6-7.6(m, 16H), 7.8-8.1(m, 1H), 11.0-11.5(m, 2H) MS(EI):                     105(43%), 510(0.7%), 524(0.9%), 553(M.sup.+ -CO.sub.2, 7%)      44                                                                                ##STR64## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.95(t, J=7Hz,                       3H), 1.3-1.9(m, 2H), 2.9- 3.5(m, 4H), 4.15(t, J=7Hz, 2H),                     4.16(s, 2H), 6.7-7.7(m, 17H), 7.8-8.1(m, 1H), 9.3-9.9(m,                      2H)                                                             45                                                                                ##STR65## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.93(t, J=7Hz,                       3H), 1.3-1.9(m, 2H), 2.8- 3.4(m, 4H), 3.57(s, 3H), 4.07(t,                    J=7Hz, 2H), 4.14(s, 2H), 6.65(d, J=8Hz, 4H), 7.10(s, 9H),                     7.49(d, J=8Hz, 4H), 11.2-11.7(m, 2H) MS(FAB): 614(M+H)          46                                                                                ##STR66## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.92(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 3.03 (t, J=7Hz, 2H), 3.17(t, J=7Hz,                      2H), 3.61(s, 3H), 4.16(s, 2H), 4.16(t, J=7Hz, 2H),                            6.3-8.0(m, 17H), 11.3-11.8(m, 2H) MS(EI): 105(61%),                           421(4%), 525(0.3%), 569(M.sup.+ -CO.sub.2, 0.2%)                47                                                                                ##STR67## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.96(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 3.06 (t, J=7Hz, 2H), 3.23(t, J=7Hz,                      2H), 3.76(s, 3H), 4.18(s, 2H), 4.19(t, J=7Hz, 2H),                            6.6-7.6(m, 16H), 7.7-8.0(m, 1H), 10.8-11.6(m, 2H)               48                                                                                ##STR68## MS(EI): 105(100%), 338(0.7%), 544(1%), 573(M.sup.+ -CO.sub.2                  , 4%)                                                           49                                                                                ##STR69## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.94(t, J=7Hz,                       3H), 1.2-1.9(m, 2H), 2.8- 3.4(m, 4H), 3.10(t, J=7Hz, 2H),                     3.18(s, 2H), 6.5-7.5(m, 16H), 7.7-8.0(m, 1H), 11.0-11.6(m,                    2H) MS(FAB): 618(M+H)                                           50                                                                                ##STR70## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.92(t, J=7Hz,                       3H), 1.2-1.9(m, 2H), 3.05 (t, J=7Hz, 2H), 3.18(t, J=7Hz,                      2H), 4.13(s, 2H), 4.50(t, J=7Hz, 2H), 6.6- 7.5(m, 15H),                       7.7-7.9(m, 1H), 9.3-10.0(m, 2H)                                 51                                                                                ##STR71## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.90(t, J=7Hz,                       3H), 1.3-1.8(m, 2H), 3.05 (t, J=7Hz, 2H), 3.16(t, J=7Hz,                      2H), 4.14(s, 2H), 4.25(t, J=7Hz, 2H), 6.6- 7.6(m, 15H),                       7.7-8.0(m, 1H), 10.8-11.5(m, 2H) MS(FAB): 590(M+H)              52                                                                                ##STR72## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.91(t, J=7Hz,                       3H), 1.2-1.8(m, 2H), 2.83 (t, J=7Hz, 2H), 3.15(t, J=7Hz,                      2H), 4.04(t, J=7Hz, 2H), 4.10(s, 2H), 6.8- 7.5(m, 17H),                       7.7-8.0(m, 1H), 11.0-11.6(m, 2H) MS(FAB): 598(M+H)              53                                                                                ##STR73## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.90(t, J=7Hz,                       3H), 1.3-1.9(m, 2H), 3.08 (t, J=7Hz, 2H), 3.11(t, J=7Hz,                      2H), 3.42(d, J=6Hz, 2H), 4.08(s, 2H), 4.18 (t, J=7Hz, 2H),                    4.5-5.1(m, 2H), 5.3-6.0(m, 1H), 6.8-7.6(m, 12H), 7.7-                         8.0(m, 1H), 10.1-10.7(m, 2H) MS(FAB): 548(M+H)                  54                                                                                ##STR74## .sup.1 H NMR(CDCl.sub.3, 60MHz): δ 0.90(t, J=7Hz,                       3H), 1.10(t, J=7Hz, 3H), 1.2- 1.9(m, 2H), 3.05(t, J=7Hz,                      2H), 4.1-4.4(m, 4H), 4.20(s, 2H), 6.9-7.5 (m, 18H) MS(FAB):                   612(M+H)                                                        55 NH.sup.n Pr                                                                              .sup.1 H NMR(CDCl.sub.3 +10%CD.sub.3 OD, 60MHz): δ                      0.90(t, J=7Hz, 3H), 1.0-1.7                                                   (m, 6H), 2.92(t, J=7Hz, 2H), 3.07(t, J=7Hz, 2H), 4.09(t,                      J=7Hz, 2H), 4.23                                                              (s, 2H), 6.7-7.9(m, 13H)                                                      MS(EI): 105(84%), 299(0.8%), 534(M.sup.+ -CO.sub.2,             __________________________________________________________________________                  9%)                                                              *Synthesis Example No.                                                   

SYNTHESIS EXAMPLES 56 TO 71

The following compounds were synthesized by converting correspondingcompounds into their potassium salts in the same manner as in SynthesisExample 4.

    ______________________________________                                         ##STR75##                                                                    No.* R.sup.3           FAB-MS                                                 ______________________________________                                        56   Cl                MS(FAB): 618(M+H)                                      57   I                 MS(FAB): 710(M+H)                                      58                                                                                  ##STR76##        MS(FAB): 630(M-CO.sub.2 +H)                            59                                                                                  ##STR77##        MS(FAB): 674(M+H)                                      60                                                                                  ##STR78##        MS(FAB): 674(M+H)                                      61                                                                                  ##STR79##        MS(FAB): 616(M-CO.sub.2 +H)                            62                                                                                  ##STR80##        MS(FAB): 690(M+H)                                      63                                                                                  ##STR81##        MS(FAB): 690(M+H)                                      64                                                                                  ##STR82##        MS(FAB): 690(M+H)                                      65                                                                                  ##STR83##        MS(FAB): 650(M-CO.sub.2 +H)                            66                                                                                  ##STR84##        MS(FAB): 694(M+H)                                      67                                                                                  ##STR85##        MS(FAB): 739(M+H)                                      68                                                                                  ##STR86##        MS(FAB): 666(M+H)                                      69                                                                                  ##STR87##        MS(FAB): 674(M+H)                                      70                                                                                  ##STR88##        MS(FAB): 624(M+H)                                      71                                                                                  ##STR89##        MS(FAB): 688(M+H)                                      72   NH.sup.n Pr       MS(FAB): 611(M-CO.sub.2 +H)                            ______________________________________                                         *Synthesis Example No.                                                   

EXPERIMENTAL EXAMPLE 1

Test for Antagonistic Effect against Angiotensin:

A rabbit was sacrificed while anesthetized with pentobarbital, andimmediately its thoracic aorta was removed. This was cut into a ringspecimen, kept at 37° C. and hung in a nutrient liquid (Krebs-Henseleitsolution) aerated with a mixed gas comprising 95% oxygen and 5% carbondioxide, whereupon its isometric contraction was measured. The specimenwas equilibrated for one hour, with replacement of the nutrient liquidevery 20 minutes, and thereafter angiotensin II (AngII: 10⁻⁸ M) wasapplied thereto to cause its contraction. To evaluate the effect of thecompounds of the present invention, the compound to be tested (10⁻⁷ M or10⁻⁸ M) was applied as pre-treatment to the specimen in 20 minutesbefore the fourth application of AngII thereto, the percentage ofinhibiting the contraction caused by AngII was obtained on the basis ofthe third contraction caused by AngII of being 100%. The percentage wascorrected, using dimethylsulfoxide (DMSO).

                  TABLE 6                                                         ______________________________________                                        Percentage of Inhibition of Contraction (%)                                   Compound of the Invention                                                     (as the number of                                                             Synthesis Example)                                                                             1 × 10.sup.-7 M                                                                   1 × 10.sup.-8 M                              ______________________________________                                         4               85        40                                                 56               84        51                                                 61               77        34                                                 64               92        29                                                 67               35        13                                                 68               35        18                                                 71               36        14                                                 72               15         7                                                 ______________________________________                                    

EXPERIMENTAL EXAMPLE 2

Test for Hypotensive Effect

The compounds of the present invention to be tested were dissolved in aphysiological saline solution and was orally administered to aspontaneous hypertensive male rat (10-week age). The blood pressure ofthe rat was measured, via a pressure transducer through the catheterthat had previously been introduced into its aorta from its femoralartery. The variation in the blood pressure was observed from before theapplication of the compound to 20 hours after the application thereof.

The following table shows the dose of the compound administered, thelargest percentage of the depression of the blood pressure and the timeafter the administration at which the largest percentage was obtained.

                  TABLE 7                                                         ______________________________________                                                                Largest                                               Compound of the         Percentage                                            Invention (as the       of Blood                                              number of Synthesis                                                                        Dose       Pressure  Time                                        Example)     (mg/kg)    Depression                                                                              (hr)                                        ______________________________________                                        4            30         29.6      10                                          ______________________________________                                    

EXPERIMENTAL EXAMPLE 3

Test for Inhibition of Binding to Angiotensin II (AT₂) Receptor:

The effect of the compounds of the present invention for inhibiting thebinding activity of Angiotensin II (AngII) to the bovine brain receptorwere tested, according to the method by J. P. Bennett, Jr. et al. J.Biol. Chem., 251, 7423-7430 (1976)!.

10⁻⁶ M of the compound of the present invention to be tested was addedto an aqueous solution containing a predetermined amount of a bovinebrain specimen and 0.1 nM of ¹²⁵ I-AngII and incubated at 37° C. for 30minutes. The resulting solution was separated through a glass fiberfilter to terminate the reaction. The radioactivity bonded to the filterwas quantified by a γ-counter.

                  TABLE 8                                                         ______________________________________                                        Compound of the Invention                                                     (as the number of Percentage of                                               Synthesis Example)                                                                              Inhibition (%)                                              ______________________________________                                        4                 55.1                                                        ______________________________________                                         Formulation Examples!                                                        FORMULATION EXAMPLE 1:                                                        Tablets:                                                                      Compound (produced in                                                         Synthesis Example 4)                                                                              10         g                                              Lactose             260        g                                              Crystal cellulose powder                                                                          600        g                                              Corn Starch         350        g                                              Hydroxypropyl cellulose                                                                           100        g                                              CMC-Ca              150        g                                              Magnesium stearate  30         g                                              Total               1,500      g                                              ______________________________________                                    

The above-mentioned components were mixed by a usual method and thentabletted to produce 10,000 sugar-coated tablets each containing one mgof the active ingredient.

FORMULATION EXAMPLE 2

Capsules:

    ______________________________________                                        Compound (produced in                                                                           10          g                                               Synthesis Example 4)                                                          Lactose           440         g                                               Crystal cellulose powder                                                                        1,000       g                                               Magnesium stearate                                                                              50          g                                               Total             1,500       g                                               ______________________________________                                    

The above-mentioned components were mixed by a usual method and thenpacked in gelatin capsules to obtain 10,000 capsules each containing onemg of the active ingredient.

FORMULATION EXAMPLE 3

Soft Capsules:

    ______________________________________                                        Compound (produced in                                                                           10          g                                               Synthesis Example 4)                                                          PEG400            479         g                                               Saturated fatty acid                                                                            1,500       g                                               triglyceride                                                                  Peppermint Oil    1           g                                               Polysorbate 80    10          g                                               Total             2,000       g                                               ______________________________________                                    

The above-mentioned components were mixed and encapsulated into No. 3soft gelatin capsules by a usual method to obtain 10,000 soft capsuleseach containing one mg of the active ingredient, by an ordinary method.

FORMULATION EXAMPLE 4

Ointment:

    ______________________________________                                        Compound (produced in                                                                           1.0         g                                               Synthesis Example 4)                                                          Liquid paraffin   10.0        g                                               Cetanol           20.0        g                                               White vaseline    68.4        g                                               Ethylparaben      0.1         g                                               1-Menthol         0.5         g                                               Total             100.0       g                                               ______________________________________                                    

The above-mentioned components were mixed by a usual method to obtain 1%ointment.

FORMULATION EXAMPLE 5

Suppositories:

    ______________________________________                                        Compound (produced in                                                                           1           g                                               Synthesis Example 4)                                                          Witepsol H15*     478         g                                               Witepsol W35*     520         g                                               Polysorbate 80    1           g                                               Total             1,000       g                                               ______________________________________                                         *Trade name for triglyceride compound                                    

The above-mentioned components were melt-mixed by a usual method andpoured into suppository containers, followed by cooling forsolidification to obtain 1,000 suppositories of one g each containingone mg of the active ingredient.

Industrial Applicability

The compounds of the present invention have an antagonistic effectagainst angiotensin II and are useful for prevention and remedy ofhypertension, congestive cardiac insufficiency, chronic renalinsufficiency, aldosteronism, hyper-intraocular pressure, etc.

We claim:
 1. Pyrazole compounds of the following general formula (1),and their tautomers and salts: ##STR90## wherein R¹ represents ahydrogen atom, a C₁ -C₁₀ alkyl group (said alkyl group is unsubstitutedor substituted by one or more substituents selected from a halogen atom,a hydroxyl group and a C₁ -C₁₀ alkoxy group), a C₂ -C₁₀ alkenyl group(said alkenyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group and a C₁-C₁₀ alkoxy group), a C₂ -C₁₀ alkynyl group (said alkynyl group isunsubstituted or substituted by one or more substituents selected from ahalogen atom, a hydroxyl group and a C₁ -C₁₀ alkoxy group), a C₃ -C₁₀cycloalkyl group (said cycloalkyl group is unsubstituted or substitutedby one or more substituents selected from a halogen atom, a hydroxylgroup and a C₁ -C₁₀ alkoxy group), a C₃ -C₁₀ cycloalkenyl group (saidcycloalkenyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group and a C₁-C₁₀ alkoxy group) or a C₆ -C₁₀ aromatic group (said aromatic group isunsubstituted or substituted by one or more substituents selected from aC₁ -C₁₀ alkyl group, a halogen atom, a hydroxyl group and a C₁ -C₁₀alkoxy group);R² represents COX¹ R¹², wherein R¹² represents a hydrogenatom or a C₁ -C₁₀ alkyl group and X¹ represents an oxygen atom or asulfur atom; R³ represents a C₁ -C₁₀ acyl group; R⁴, R⁵ and R⁶ eachindependently represents a hydrogen atom, a halogen atom, a hydroxylgroup or a C₁ -C₁₀ alkyl group; R⁷ represents a 5-tetrazolyl group, Xrepresents a nitrogen atom, Y and Z each independently represent CR⁴⁰,wherein R⁴⁰ represents a hydrogen atom, a halogen atom or a C₁ -C₁₀alkyl group; A represents (CR⁴¹ R⁴¹ ')m⁷, wherein m⁷ represents 0, 1, 2or 3, and R⁴¹ and R⁴¹ ' each independently represents a hydrogen atom ora C₁ -C₁₀ alkyl group; D represents a C₆ -C₁₀ aromatic group, whereinsaid aromatic group is unsubstituted or mono-substituted topenta-substituted by a halogen atom or a C₁ -C₁₀ alkyl group; Erepresents CR⁵² R⁵³, wherein R⁵² and R⁵³ each independently represents ahydrogen atom or a C₁ -C₁₀ alkyl group; and G represents a covalentbond.
 2. Pyrazole compounds and their tautomers and salts as claimed inclaim 1, wherein R¹ represents a C₁ -C₁₀ alkyl group (said alkyl groupis unsubstituted or substituted by one or more substituents selectedfrom a halogen atom, a hydroxyl group and a C₁ -C₁₀ alkoxy group), a C₂-C₁₀ alkenyl group (said alkenyl group is unsubstituted or substitutedby one or more substituents selected from a halogen atom, a hydroxylgroup and a C₁ -C₁₀ alkoxy group) or a C₃ -C₁₀ cycloalkyl group (saidcycloalkyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group and a C₁-C₁₀ alkoxy group).
 3. Pyrazole compounds and their tautomers and saltsas claimed in claim 2, wherein R² represents COX¹ R¹², wherein R¹²represents a hydrogen atom or a straight chain or branched C₁ -C₁₀ alkylgroup (said akyl group is unsubstituted or substituted by one or moresubstituents selected from a halogen atom, a hydroxyl group and a C₁-C₁₀ alkoxy group), and X¹ represents an oxygen atom;R⁴, R⁵ and R⁶ arehydrogen atoms; and E represents CH₂.
 4. A liquid compound for treatmentof one or more of hypertension, congestive cardiac insufficiency, andchronic renal insufficiency, said compound containing at least one ofpyrazole compounds and their tautomers and salts as claimed in claim 1,and at least one compound selected from the group consisting ofsolvents, surfactants, suspending agents and preservatives.
 5. Pyrazolecompounds and their tautomers and salts as claimed in claim 3, whereinR¹ represents a C₁ -C₁₀ alkyl group; and Y and Z each represent CH. 6.Pyrazole compounds and their tautomers and salts as claimed in claim 5,wherein D represents a phenyl group (said phenyl group is unsubstitutedor substituted by one or more substituents selected from a halogen atomand a C₁ -C₁₀ alkyl group).
 7. Pyrazole compounds and their tautomersand salts as claimed in claim 6, wherein R² represents a carboxyl group.8. A composition for treating one or more of hypertension, congestivecardiac insufficiency, and chronic renal insufficiency, said compositioncontaining at least one of pyrazole compounds and their tautomers andsalts as claimed in claim 1, and at least one compound selected from thegroup consisting of excipients, binders, disintegrators, lubricants andsmoothers.